370 results match your criteria Drug Development Research[Journal]


Further modifications of 1H-pyrrolo[2,3-b]pyridine derivatives as inhibitors of human neutrophil elastase.

Drug Dev Res 2019 Apr 19. Epub 2019 Apr 19.

Department of Microbiology and Immunology, Montana State University, Bozeman, Montana.

Human neutrophil elastase (HNE) is a potent protease that plays an important physiological role in many processes and is considered to be a multifunctional enzyme. HNE is also involved in a variety of pathologies affecting the respiratory system. Thus, compounds able to inhibit HNE proteolytic activity could represent effective therapeutics. Read More

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http://dx.doi.org/10.1002/ddr.21539DOI Listing

Synthesis, in vivo anticonvulsant testing, and molecular modeling studies of new nafimidone derivatives.

Drug Dev Res 2019 Apr 11. Epub 2019 Apr 11.

Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Hacettepe University, Ankara, Turkey.

An estimated 50 million people suffer epilepsy worldwide and 30% of the cases do not respond to current antiepileptic drugs (AEDs). Here, we report synthesis and anticonvulsant screening of new derivatives of nafimidone, a well-known member of (arylakyl)azole anticonvulsants. The compounds showed promising protection against maximal electroshock (MES)-induced seizures in mice and rats when administered via intraperitoneal (ip) and oral route. Read More

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http://dx.doi.org/10.1002/ddr.21538DOI Listing
April 2019
1 Read

Anti-inflammatory effects of Vicenin-2 on dextran sulfate sodium-induced colitis in mice.

Drug Dev Res 2019 Apr 10. Epub 2019 Apr 10.

Anorectal of Traditional Chinese Medicine, Shandong Provincial Hospital Affiliated to Shandong University, Huaiyin District, Jinan, Shandong Province, China.

The objective of the present work was to evaluate the anti-inflammatory effects of Vicenin-2 on dextran sulfate sodium (DSS)-induced colitis model. Colitis was induced in C57BL/6J mice by administration of 2% DSS in drinking water for 7 days. In addition to DSS, Vicenin-2 (50 mg kg /day ) was administrated orally to the test group. Read More

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http://dx.doi.org/10.1002/ddr.21529DOI Listing

Synthesis, characterization, molecular docking evaluation, antidepressant, and anti-Alzheimer effects of dibenzylidene ketone derivatives.

Drug Dev Res 2019 Apr 9. Epub 2019 Apr 9.

Basic Sciences Department, College of Science and Health Professions, King Saud bin Abdulaziz University for Health Sciences, Ministry of National Guard Health Affairs, Jeddah, Kingdom of Saudi Arabia.

Novel bioactive compounds as synthetic analogs of the potent herbal medicines can be optimized as potential drug candidates for various neurologic disorders. This study was performed to investigate the newly synthesized dibenzylidene ketone derivatives: (2E,6E)-2,6-dibenzylidene cyclohexanone (A1K1) and (1E,4E)-5-(2,3-dichlorophenyl)-1-(4-methoxyphenyl)-2-methylpenta-1,4-diene-3-one (A2K2) and evaluate its potential anti-Alzheimer's and anti-depressant properties. Both the derivatives are chemically characterized by using HNMR and CNMR techniques. Read More

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http://dx.doi.org/10.1002/ddr.21537DOI Listing

Pharmacodynamic interaction of 3α-hydroxymasticadienonic acid and diligustilide against indomethacin-induced gastric damage in rats.

Drug Dev Res 2019 Apr 8. Epub 2019 Apr 8.

Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, Ciudad Universitaria, Ciudad de México, Mexico.

The aims of the study were to evaluate the pharmacodynamic interaction between 3α-hydroxymasticadienonic acid and diligustilide (DLG), isolated from the plants Amphiptherygium adstringens and Ligusticum porteri, respectively, using the indomethacin-induced gastric injury model, as well as their individual gastroprotective efficacy in this model. Male Wistar rats were orally administered with 3α-hydroxymasticadienonic acid, DLG or the mixture of 3α-hydroxymasticadienonic acid-DLG (at a fixed-ratio combination of 1:1, 1:3, and 3:1). Thirty minutes later, the gastric damage was induced by a single oral dose of indomethacin (30 mg/kg). Read More

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http://dx.doi.org/10.1002/ddr.21535DOI Listing

Glycitein induces reactive oxygen species-dependent apoptosis and G0/G1 cell cycle arrest through the MAPK/STAT3/NF-κB pathway in human gastric cancer cells.

Drug Dev Res 2019 Mar 27. Epub 2019 Mar 27.

Department of Food Science and Engineering, College of Food Science, Heilongjiang Bayi Agricultural University, Daqing, Heilongjiang, China.

Glycitein is an isoflavone that reportedly inhibits the proliferation of human breast cancer and prostate cancer cells. However, its anti-cancer molecular mechanisms in human gastric cancer remain to be defined. This study evaluated the antitumor effects of glycitein on human gastric cancer cells and investigated the underlying mechanisms. Read More

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http://dx.doi.org/10.1002/ddr.21534DOI Listing
March 2019
1 Read

Cerebrolysin improves peripheral inflammatory pain: Sex differences in two models of acute and chronic mechanical hypersensitivity.

Drug Dev Res 2019 Mar 25. Epub 2019 Mar 25.

KWS BioTest, Department of Pharmacology, Portishead, Somerset, UK.

Chronic inflammatory pain is a major health problem worldwide with high prevalence in women. Cerebrolysin is a multimodal neuropeptide preparation that crosses the blood brain barrier and displays neuroprotective properties in aging and disease. Previously, we showed that cerebrolysin reduced mechanical allodynia in a model of persistent inflammation and pain. Read More

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http://dx.doi.org/10.1002/ddr.21528DOI Listing

Efficacy of targeted liposomes and nanocochleates containing imatinib plus dexketoprofen against fibrosarcoma.

Drug Dev Res 2019 Mar 22. Epub 2019 Mar 22.

Department of Preclinical Sciences, OndokuzMayıs University, Faculty of Veterinary Medicine, Samsun, Turkey.

The main challenges in treating cancer using chemotherapeutics are insufficient dose at the target site and the development of drug resistance, while higher doses can induce side effects by damaging nontarget tissues. Combinatorial drug therapy may overcome these limitations by permitting lower doses and more specific targeting, thereby mitigating drug resistance and nontarget side effects. Recent reports indicate that nonsteroidal anti-inflammatory drugs (NSAIDs) have anticancer potential and can be used together with conventional chemotherapeutics to improve efficacy and safety. Read More

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http://dx.doi.org/10.1002/ddr.21530DOI Listing
March 2019
2 Reads

Near-infrared imaging of diseases: A nanocarrier approach.

Drug Dev Res 2019 Mar 20. Epub 2019 Mar 20.

Department of Radiopharmacy, Faculty of Pharmacy, Hacettepe University, Sıhhiye, Ankara, Turkey.

Developments in fluorescence imaging, brought popularity to near infrared (NIR) imaging with far-red and NIR fluorophores applied for biosensing and bioimaging in living systems. Noninvasive NIR imaging gained popularity with the use of effective NIR dyes to obtain macroscopic fluorescence images. Several attributes of NIR dyes make them desirable agents, including high specificity, high sensitivity, minimized background interference, and the ability to easily conjugate with drug delivery systems. Read More

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http://dx.doi.org/10.1002/ddr.21532DOI Listing

8-Hydroxyquinolines are bactericidal against Mycobacterium tuberculosis.

Drug Dev Res 2019 Mar 20. Epub 2019 Mar 20.

TB Discovery Research, Infectious Disease Research Institute, Seattle, Washington.

There is an urgent need for new treatments effective against Mycobacterium tuberculosis, the causative agent of tuberculosis. The 8-hydroxyquinoline series is a privileged scaffold with anticancer, antifungal, and antibacterial activities. We conducted a structure-activity relationship study of the series regarding its antitubercular activity using 26 analogs. Read More

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http://dx.doi.org/10.1002/ddr.21531DOI Listing
March 2019
1 Read

Phloroglucinol averts isoprenaline hydrochloride induced myocardial infarction in rats.

Drug Dev Res 2019 Mar 19. Epub 2019 Mar 19.

Department of Cardiology, The Second Affiliated Hospital of Xi'an Jiaotong University, No 157 Xiwulu,Xincheng District, Xi'an City, Shaanxi Province, China.

Myocardial infarction (MI) is indicated by the symptoms like sharp chest pain, sweating, palpitations, and nervousness finally leading to heart attack. MI occurs mainly due to the risk factors like smoking, elevated blood pressure, diabetes, hypercholesterolemia, obesity, decreased HDL level, elevated LDL level, hyperlipoproteinemia and aging consequently leads to demandable coronary blood supply, oxidative stress, and acute necrosis of the myocardium. Cardioprotective potential of the phloroglucinol (PG) was assessed by treating isoprenaline hydrochloride (ISO; 85 mg/kg b. Read More

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http://dx.doi.org/10.1002/ddr.21517DOI Listing
March 2019
2 Reads

The protective effect of kaempferol on heart via the regulation of Nrf2, NF-κβ, and PI3K/Akt/GSK-3β signaling pathways in isoproterenol-induced heart failure in diabetic rats.

Drug Dev Res 2019 Mar 12. Epub 2019 Mar 12.

Medical Research and Laboratory Diagnostic Center, Jinan Central Hospital Affiliated to Shandong University, Jinan, People's Republic of China.

This study was designed to delineate the effect of kaempferol (KF) on heart failure (HF) in diabetic rats. Streptozotocin-induced male diabetic rats received KF orally at 10 and 20 mg/kg for 42 consecutive days. In last 2 days of the experimental period, isoproterenol was subcutaneously injected at 85 mg/kg to induce HF. Read More

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http://dx.doi.org/10.1002/ddr.21495DOI Listing
March 2019
3 Reads

Cristazine, a novel dioxopiperazine alkaloid, induces apoptosis via the death receptor pathway in A431 cells.

Drug Dev Res 2019 Mar 12. Epub 2019 Mar 12.

Department of Microbiology, College of Natural Sciences, Pukyong National University, Busan, Republic of Korea.

The fungus Chaetomium sp. is a causative agent of infections in humans and is ubiquitous in the natural environment. The secondary metabolites of this genus exhibit many biological activities, including antifungal activity and toxicity in mitochondria. Read More

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http://dx.doi.org/10.1002/ddr.21527DOI Listing
March 2019
1 Read

What lurks in the shadows of the openness hyperbole for biopharmaceuticals?

Drug Dev Res 2019 Mar 11. Epub 2019 Mar 11.

Centre for Advanced Studies in Bio-Medical Innovation Law (CeBIL), University of Copenhagen, Copenhagen S, Denmark.

Recent advances in transparency initiative signify laudable developments. Yet, a closer look on the legal developments indicates that commercially confidential information and personal data will continue to pose persisting challenges for clinical trial transparency and drug development. This article depicts these developments with a particular focus on European Medicines Agency (EMA) and Biologics. Read More

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http://dx.doi.org/10.1002/ddr.21526DOI Listing

Transcriptome analysis predicts mode of action of benzimidazole molecules against Staphylococcus aureus UAMS-1.

Drug Dev Res 2019 Feb 21. Epub 2019 Feb 21.

Department of Chemistry, School of Natural Sciences, Shiv Nadar University, Dadri, Uttar Pradesh, India.

Antimicrobial drug resistance is one of the most critical problems that plagued the human race in modern times. Discovery of novel antibiotics is important to counter this threat. Accordingly, herein we have reported the discovery of substituted benzimidazole class of molecules with antimicrobial property (specifically against Staphylococcus aureus). Read More

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http://dx.doi.org/10.1002/ddr.21523DOI Listing
February 2019

Stilbene derivatives as new perspective in antifungal medicinal chemistry.

Drug Dev Res 2019 Feb 20. Epub 2019 Feb 20.

Dipartimento di Farmacia, Università "G. d'Annunzio", Chieti, Italy.

The high incidence and mortality of invasive fungal infections and serious drug resistance have become a global public health issue. There is an urgent need for alternative antimicrobials to control fungal infections and targeting it by antifungal substances from the natural sources represents a promising new strategy for the development of novel antifungal agents. Resveratrol (3,5,4'-trihydroxy-trans-stilbene) is a phytoalexin produced by plant species in response to environmental stress or pathogenic attacks. Read More

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http://dx.doi.org/10.1002/ddr.21525DOI Listing
February 2019
2 Reads

Pharmacological interaction between NSAIDS with clomipramine and risperidone in mice visceral pain.

Drug Dev Res 2019 Feb 14. Epub 2019 Feb 14.

Department of Pharmacology, Faculty of Medicine, Pharmacology Program, ICBM, Universidad de Chile, Santiago, Chile.

Nonsteroidal anti-inflammatory drugs (NSAIDs) possess as primary action mechanism the inhibition of cyclooxygenases (COX-1, COX-2, and COX-3), thus producing a decreasing prostaglandin synthesis. This study was designed to evaluate whether the antinociception induced by NSAIDs could be modulated by clomipramine or risperidone using a chemical model of inflammatory acute visceral pain, the abdominal acetic acid induced a writhing test in mice. Dose-response curves, intraperitoneal, or intrathecal for the antinociceptive activity displayed by ketoprofen, piroxicam, nimesulide, parecoxib, and paracetamol were analyzed in order to obtain the ED of each drug. Read More

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http://dx.doi.org/10.1002/ddr.21519DOI Listing
February 2019

Ilexgenin A inhibits mitochondrial fission and promote Drp1 degradation by Nrf2-induced PSMB5 in endothelial cells.

Drug Dev Res 2019 Feb 14. Epub 2019 Feb 14.

State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing, China.

Atherosclerosis (AS) is one of important events involving in the pathological process of coronary artery disease. Many traditional Chinese medicines have been widely used for the treatment of AS. Previous studies have demonstrated that Ilexgenin A (IA) obtained from Ilex hainanensis Merr. Read More

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http://dx.doi.org/10.1002/ddr.21521DOI Listing
February 2019
2 Reads
0.734 Impact Factor

Anti-neuroinflammatory effects of tannic acid against lipopolysaccharide-induced BV2 microglial cells via inhibition of NF-κB activation.

Drug Dev Res 2019 03 6;80(2):262-268. Epub 2019 Feb 6.

Department of Neurosurgery, The Second People's Hospital of Yunnan Province, Kunming, Yunnan, China.

Microglia mediated neuroinflammation is known to cause various neurodegenerative and neurological ailments. Tannic acid is a natural polyphenol which has been reported to possess antioxidant, anti-inflammatory, anticarcinogenic, antimutagenic, antitumor, and antimicrobial activities. As there are no reports till date on the anti-neuroinflammatory effects of tannic acid, this study was conducted to analyze the possible mechanism and pathway involved in the prevention of neuroinflammation by tannic acid in BV2 microglial cells. Read More

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http://dx.doi.org/10.1002/ddr.21490DOI Listing
March 2019
3 Reads

Protective role of sitagliptin against oxidative stress in a kainic acid-induced status epilepticus in rats models via Nrf2/HO-1 pathway.

Drug Dev Res 2019 Feb 4. Epub 2019 Feb 4.

Biotech Center for Viral Disease Emergency, National Institute for Disease Control and Prevention, Chinese Disease Control and Prevention, Beijing, China.

Preclinical Research & Development Aim: Sitagliptin (Sita) is a dipeptidyl peptidase-4 inhibitor which has been approved as a curing medicine for Type 2 diabetes (T2D) and has also reported its neuroprotective and antioxidant activity. This article describes the therapeutic effects of Sita on induced rat model of SE by kainic acid (KA) and investigated the antioxidative pathway of sita.

Methods: Sprague-Dawley male rats were used randomly divided in four groups: vehicle control, KA and Sita + KA in a 5 and 10 mg/kg doses respectively in further groups. Read More

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http://dx.doi.org/10.1002/ddr.21516DOI Listing
February 2019

Can acetaminophen/dimethyl sulfoxide formulation prevent accidental and intentional acetaminophen hepatotoxicity?

Drug Dev Res 2019 Jan 30. Epub 2019 Jan 30.

Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia.

An overdose of acetaminophen (APAP) causes liver injury in experimental animals and humans. The activation step (formation of reactive metabolite, N-acetyl-p-benzoquinone imine by cytochrome P450 system) and the consequent downstream pathway of oxidative stress, nitrosative stress, and inflammation play an important role in APAP-induced hepatotoxicity. Formulation of APAP with an inhibitor of the activation step would be ideal to prevent accidental and intentional APAP toxicity. Read More

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http://dx.doi.org/10.1002/ddr.21520DOI Listing
January 2019
3 Reads
0.734 Impact Factor

Mechanisms underlying isoliquiritigenin-induced apoptosis and cell cycle arrest via ROS-mediated MAPK/STAT3/NF-κB pathways in human hepatocellular carcinoma cells.

Drug Dev Res 2019 Jan 30. Epub 2019 Jan 30.

Department of Biochemistry and Molecular Biology, College of Life Science & Technology, Heilongjiang Bayi Agricultural University, Daqing, China.

Hit, Lead & Candidate Discovery Isoliquiritigenin (ISL), a natural flavonoid isolated from plant licorice, has various pharmacological properties, including anticancer, anti-inflammatory, and antiviral effects. However, the underlying mechanisms and signaling pathways of ISL in human hepatocellular carcinoma (HCC) cells remain unknown. In this study, we evaluated the effects of ISL on the apoptosis of human HCC cells with a focus on reactive oxygen species (ROS) production. Read More

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http://doi.wiley.com/10.1002/ddr.21518
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http://dx.doi.org/10.1002/ddr.21518DOI Listing
January 2019
16 Reads
0.734 Impact Factor

Anticonvulsant evaluation and docking analysis of VV-Hemorphin-5 analogues.

Drug Dev Res 2019 Jan 25. Epub 2019 Jan 25.

Department of Behavioral Neurobiology, Institute of Neurobiology, Bulgarian Academy of Sciences, Sofia, Bulgaria.

Preclinical Research & Development VV-Hemorphin-5 is an endogenous opioid peptide of the Hemorphin family with affinity at opioid receptors. A series of C-amide analogues have been synthesized, based on the structure of VV-Hemorphin-5, modified at position 1 and 7 by the un/natural amino acids (Aa8-Val-Val-Tyr-Pro-Trp-Thr-Gln-NH and Val-Val-Tyr-Pro-Trp-Thr-Aa1-NH ) using SPPS, Fmoc-chemistry. The peptide derivatives were evaluated for their anticonvulsant activity in three acute seizure tests in male ICR mice, the maximal electroshock (MES), the 6 Hz psychomotor seizure test, and the timed intravenous pentylenetetrazole (ivPTZ) infusion test. Read More

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http://doi.wiley.com/10.1002/ddr.21514
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http://dx.doi.org/10.1002/ddr.21514DOI Listing
January 2019
1 Read

Structure-activity study of fluorine or chlorine-substituted cinnamic acid derivatives with tertiary amine side chain in acetylcholinesterase and butyrylcholinesterase inhibition.

Drug Dev Res 2019 Jan 24. Epub 2019 Jan 24.

College of Medicine, Hu'nan Normal University, Changsha, China.

Hit, Lead & Candidate Discovery In this study, a series of new fluorine or chlorine-substituted cinnamic acid derivatives that contain tertiary amine side chain were designed, synthesized, and evaluated in acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition. The results show that almost all the derivatives containing tertiary amine side chain (compounds 4a-9d) exhibit moderate or potent activity in AChE inhibition. By contrast, their parent compounds (compounds 3a-3f) in the absence of tertiary amine moitery exhibit poor inhibitory activity against AChE. Read More

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http://dx.doi.org/10.1002/ddr.21515DOI Listing
January 2019

Curcumin reduces inflammation in knee osteoarthritis rats through blocking TLR4 /MyD88/NF-κB signal pathway.

Authors:
Yun Zhang Yu Zeng

Drug Dev Res 2019 Jan 21. Epub 2019 Jan 21.

Department of Hyperbaric Oxygen, Sichuan Academy of Medical Sciences & Sichuan Provincial People's Hospital, Chengdu, China.

Preclinical Research & Development Curcumin has been shown to possess a series of beneficial effects, such as antiinflammatory, antioxidant, analgesic, and promoting healing. However, the effect and relative mechanism of curcumin on knee osteoarthritis (OA) have not been elucidated. The aim of this study is to explore the protective effect of curcumin on monosodium iodoacetate (MIA)-induced OA. Read More

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http://doi.wiley.com/10.1002/ddr.21509
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http://dx.doi.org/10.1002/ddr.21509DOI Listing
January 2019
10 Reads

Inhibition of angiogenesis and tumor growth by a novel 1,4-naphthoquinone derivative.

Drug Dev Res 2019 Jan 11. Epub 2019 Jan 11.

Department of Immunobiology, School of Pharmacy and Pharmaceutical Sciences, Mukogawa Women's University, Nishinomiya, Hyogo, Japan.

Hit, Lead & Candidate Discovery Antiangiogenesis therapy is a promising way for treatment of solid cancers, and many angiogenesis inhibitors that target vascular endothelial growth factor (VEGF) or its receptors have been developed. We explored novel antiangiogenic compounds other than anti-VEGF drugs by screening our synthetic compound library and found that 6-thiophen-3-yl-2-methoxy-1,4-naphthoquinone (6-TMNQ) had potential as a novel angiogenesis inhibitor. This paper describes the effects of 6-TMNQ on angiogenesis and tumor growth in vitro and in vivo. Read More

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http://doi.wiley.com/10.1002/ddr.21513
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http://dx.doi.org/10.1002/ddr.21513DOI Listing
January 2019
13 Reads

Investigation of the antibacterial and antifungal activity of thiolated naphthoquinones.

Drug Dev Res 2019 Jan 4. Epub 2019 Jan 4.

Phytomedicine Programme, Department of Paraclinical Sciences, Faculty of Veterinary Sciences, University of Pretoria, Onderstepoort, South Africa.

The WHO has stated that antibiotic resistance is escalating to perilously high levels globally and that traditional therapies of antimicrobial drugs are futile against infections caused by resistant microorganisms. Novel antimicrobial drugs are therefore required. We report in this study on the inhibitory activity of the 1,4-naphthoquinone-2,3-bis-sulfides and 1,4-naphthoquinone sulfides against two bacteria and a fungus to determine their antimicrobial properties. Read More

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http://doi.wiley.com/10.1002/ddr.21512
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http://dx.doi.org/10.1002/ddr.21512DOI Listing
January 2019
2 Reads

Protective effects of quercetin against inflammation and oxidative stress in a rabbit model of knee osteoarthritis.

Drug Dev Res 2019 Jan 4. Epub 2019 Jan 4.

Department of Orthopedics, The First People's Hospital of Yongkang, Jinhua, China.

Hit, Lead & Candidate Discovery This study investigated the effects of a natural phenolic compound quercetin on surgical-induced osteoarthritis (OA) in rabbits. Forty-eight New Zealand White rabbits were used to establish OA model by Hulth modified method, and subsequently randomized into untreated OA group (treatment was drinking water), celecoxib treated group (celecoxib 100 mg kg by gavage), and quercetin treated group (25 mg kg by gavage). Sixteen nonoperated rabbits served as the normal controls (drinking water was given). Read More

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http://doi.wiley.com/10.1002/ddr.21510
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http://dx.doi.org/10.1002/ddr.21510DOI Listing
January 2019
13 Reads

Graph theoretical analysis, in silico modeling, prediction of toxicity, metabolism and synthesis of novel 2-(methyl/phenyl)-3-(4-(5-substituted-1,3,4-oxadiazol-2-yl) phenyl) quinazolin-4(3H)-ones as NMDA receptor inhibitor.

Drug Dev Res 2019 Jan 4. Epub 2019 Jan 4.

Department of Pharmacology, Faculty of Pharmacy, M. S. Ramaiah University of Applied Sciences, Bengaluru, Karnataka, India.

Hit, Lead & Candidate Discovery A variety of novel 2-(methyl/phenyl)-3-(4-(5-substituted-1,3,4-oxadiazol-2-yl)phenyl) quinazolin-4(3H)-ones have been synthesized by treating 3-(4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenyl)-2-(methyl/phenyl)-quinazolin-4(3H)-one with a variety of secondary amines. Graph theoretical analysis was used in identification of drug target that is, NMDAR (N-methyl-d-aspartate receptors). The observed reports of in silico modeling and ligand based toxicity, metabolism prediction studies were encouraging us to synthesize of title compounds and evaluate their antiepileptic effects. Read More

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http://doi.wiley.com/10.1002/ddr.21511
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http://dx.doi.org/10.1002/ddr.21511DOI Listing
January 2019
8 Reads

Alignment-based design and synthesis of new antimicrobial Aurein-derived peptides with improved activity against Gram-negative bacteria and evaluation of their toxicity on human cells.

Drug Dev Res 2019 02 28;80(1):162-170. Epub 2018 Dec 28.

Department of Biology, Damghan Branch, Islamic Azad University, Damghan, Iran.

Considering the worldwide increasing prevalence of resistance to traditional antibiotics, it is necessary to find new antibiotics to deal with this issue. Recently, antimicrobial peptides (AMPs) have been proposed as new antimicrobial agents. Aureins are a family of AMPs that are isolated from Green and Golden Bell Frogs. Read More

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http://dx.doi.org/10.1002/ddr.21503DOI Listing
February 2019
1 Read

Trichomonicidal activity of a new anthraquinone isolated from the roots of Morinda panamensis Seem.

Drug Dev Res 2019 02 20;80(1):155-161. Epub 2018 Dec 20.

Posgrado de Ciencias Genómicas, Universidad Autónoma de la Ciudad de México, Mexico, D.F., Mexico.

Trichomoniasis, caused by the protozoan parasite Trichomonas vaginalis, is the most common nonviral sexually transmitted infection worldwide. Although drug treatment is available, unpleasant side effects and increased resistance to the nitroimidazole family have been documented. Hence, there is a need for the identification of new and safe therapeutic agents against T. Read More

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http://doi.wiley.com/10.1002/ddr.21504
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http://dx.doi.org/10.1002/ddr.21504DOI Listing
February 2019
22 Reads

Design, synthesis, and biological evaluation of 1,8-naphthyridine glucosamine conjugates as antimicrobial agents.

Drug Dev Res 2019 02 20;80(1):179-186. Epub 2018 Dec 20.

Department of Biotechnology, Faculty of Applied Sciences, UCSI University, Kuala Lumpur, Malaysia.

In the quest for discovering potent antimicrobial agents with lower toxicity, we envisioned the design and synthesis of nalidixic acid-D-(+)-glucosamine conjugates. The novel compounds were synthesized and evaluated for their in vitro antimicrobial activity against Gram positive bacteria, Gram negative bacteria and fungi. Cytotoxicity using MTT assay over L6 skeletal myoblast cell line, ATCC CRL-1458 was carried out. Read More

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http://doi.wiley.com/10.1002/ddr.21508
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http://dx.doi.org/10.1002/ddr.21508DOI Listing
February 2019
11 Reads

Synthesis, in vivo and in silico evaluation of novel 2,3-dihydroquinazolin-4(1H)-one derivatives as potential anticonvulsant agents.

Drug Dev Res 2018 Dec 19. Epub 2018 Dec 19.

Department of Pharmacology, Faculty of Medicine, Zagazig University, Zagazig, Egypt.

In light of the pharmacophoric structural requirements for achieving anticonvulsant activity, a series of N-(1-methyl-4-oxo-2-un/substituted-1,2-dihydroquinazolin-3[4H]-yl)benzamide (4a-g) and N-(1-methyl-4-oxo-2-un/substituted-1,2-dihydroquinazolin-3[4H]-yl)-2-phenylacetamide (4h-n) derivatives were synthesized in two steps starting from the reaction of N-methyl isatoic anhydride with the appropriate hydrazide and followed by condensation with the appropriate aldehyde. The anticonvulsant activities of the synthesized compounds were evaluated according to the anticonvulsant drug development (ADD) programme protocol. Among the synthesized compounds, 4n showed promising activity in both the maximal electroshock (MES) and pentylenetetrazole (PTZ) tests with median effective dose (ED ) values of 40. Read More

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http://dx.doi.org/10.1002/ddr.21506DOI Listing
December 2018
1 Read
0.734 Impact Factor

Biocatalytic synthesis of diaryl disulphides and their bio-evaluation as potent inhibitors of drug-resistant Staphylococcus aureus.

Drug Dev Res 2019 02 19;80(1):171-178. Epub 2018 Dec 19.

Academy of Scientific and Innovative Research (AcSIR), New Delhi, India.

Staphylococcus aureus is a WHO Priority II pathogen for its capability to cause acute to chronic infections and to resist antibiotics, thus severely impacting healthcare systems worldwide. In this context, it is urgently desired to discover novel molecules to thwart the continuing emergence of antimicrobial resistance. Disulphide containing small molecules has gained prominence as antibacterials. Read More

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http://dx.doi.org/10.1002/ddr.21507DOI Listing
February 2019
1 Read

Tadalafil: 15 years' journey in male erectile dysfunction and beyond.

Authors:
Nermin S Ahmed

Drug Dev Res 2018 Dec 13. Epub 2018 Dec 13.

Faculty of Pharmacy and Biotechnology, Department of Pharmaceutical Chemistry, German University in Cairo, Cairo, Egypt.

Hit, Lead & Candidate Discovery Tadalafil, Cialis, Eli Lilly & Co./ICOS, (6R,12aR)-6-(1,3-benzodioxol-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6] pyrido[3,4-b]indole-1,4-dione, was first discovered in 2003. It was reported to have high diastereospecificity for phosphodiesterase 5 (PDE5) inhibitions. Read More

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http://dx.doi.org/10.1002/ddr.21493DOI Listing
December 2018
13 Reads

Bedaquiline and delamanid in the treatment of multidrug-resistant tuberculosis: Promising but challenging.

Drug Dev Res 2019 02 11;80(1):98-105. Epub 2018 Dec 11.

Department of Infectious Diseases, Huashan Hospital, Fudan University, Shanghai, China.

Improving treatment outcomes in multidrug-resistant tuberculosis (MDR-TB) is partly hampered by inadequate effective antitubercular agents. Development of bedaquiline and delamanid has potentially changed the treatment landscape for MDR-TB. This review provides an update on the progress of these novel antitubercular agents. Read More

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https://onlinelibrary.wiley.com/doi/abs/10.1002/ddr.21498
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http://dx.doi.org/10.1002/ddr.21498DOI Listing
February 2019
18 Reads
0.734 Impact Factor

Whole-genome sequencing for combatting antibiotic resistance.

Authors:
David Gurwitz

Drug Dev Res 2019 02 10;80(1):3-5. Epub 2018 Dec 10.

Department of Human Molecular Genetics and Biochemistry, Sackler Faculty of Medicine, Tel-Aviv University, Tel-Aviv, Israel.

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https://onlinelibrary.wiley.com/doi/abs/10.1002/ddr.21496
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http://dx.doi.org/10.1002/ddr.21496DOI Listing
February 2019
16 Reads

Differential regulation of intestinal and hepatic CYP3A by 1α,25-dihydroxyvitamin D : Effects on in vivo oral absorption and disposition of buspirone in rats.

Drug Dev Res 2018 Dec 10. Epub 2018 Dec 10.

Department of Manufacturing Pharmacy, College of Pharmacy, Pusan National University, Busan, South Korea.

1α,25-Dihydroxyvitamin D (also called 1,25(OH) D or calcitriol) is the biologically active form of vitamin D, which functions as a ligand to the vitamin D receptor (VDR). It was previously reported that intestinal cytochrome P450 3A (CYP3A) expression was altered by 1,25(OH) D -mediated VDR activation. However, to clarify whether the change in CYP3A subfamily expression by VDR activation can affect metabolic function, further evidence is needed to prove the effect of 1,25(OH) D treatment on CYP3A-mediated drug metabolism and pharmacokinetics. Read More

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https://onlinelibrary.wiley.com/doi/abs/10.1002/ddr.21505
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http://dx.doi.org/10.1002/ddr.21505DOI Listing
December 2018
3 Reads

Evaluation of selected commercial pharmacotherapeutic drugs as potential pancreatic lipase inhibitors and antiproliferative compounds.

Drug Dev Res 2018 Dec 3. Epub 2018 Dec 3.

School of Pharmacy, University of Jordan, Amman, Jordan.

In this study, 15 commercial acidic drugs have been evaluated for pancreatic lipase (PL) inhibitory activity using an in vitro spectrophotometric method. The acidity was the basis of selection, since most PL inhibitors exhibit acidic groups and high lipophilicity. Orlistat was the robust reference agent for potency and efficacy determinations. Read More

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http://dx.doi.org/10.1002/ddr.21499DOI Listing
December 2018
4 Reads

Spontaneous mutations conferring antibiotic resistance to antitubercular drugs at a range of concentrations in Mycobacterium smegmatis.

Drug Dev Res 2019 02 3;80(1):147-154. Epub 2018 Dec 3.

Department of Biological Sciences, Benue State University, Makurdi, Benue State, Nigeria.

Mycobacteria populations can undergo mutations in their DNA sequence during replication, which if not repaired would be transferred to future generations. Earlier studies have tackled the estimation of mutation rate in mycobacteria at fixed concentrations. However, in this study, in vitro spontaneous mutations in Mycobacterium smegmatis (Msm) mc 155 (Msm) that confers resistance to some of the most important antitubercular drugs; isoniazid (INH ), rifampicin (RIF ), kanamycin (KAN ) and streptomycin (STR ) were first determined at several highly lethal concentrations, a few of which have not been previously investigated, in a fluctuation assay. Read More

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http://dx.doi.org/10.1002/ddr.21497DOI Listing
February 2019
1 Read

Mechanism of penehyclidine hydrochloride on a dysmenorrhea rat model.

Drug Dev Res 2018 Dec 3. Epub 2018 Dec 3.

Department of Gynaecology and Obstetrics, Sichuan Academy of Medical Sciences & Sichuan Provincial People's Hospital, Chengdu, Sichuan, China.

Primary dysmenorrhea affects the quality of life in young women, particularly school and work performance. This study investigated the mechanisms of penehyclidine hydrochloride (PHC) efficacy on a rat model of primary dysmenorrhea. The model was induced by injecting both estradiol benzoate and oxytocin. Read More

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http://dx.doi.org/10.1002/ddr.21500DOI Listing
December 2018
3 Reads
0.734 Impact Factor

Design and synthesis of simplified speciophylline analogues and β-carbolines as active molecules against Plasmodium falciparum.

Drug Dev Res 2019 02 29;80(1):133-137. Epub 2018 Nov 29.

Aix Marseille Univ, CNRS, Centrale Marseille, iSm2, France.

A structure-activity relationship study of active molecules against chloroquine-resistant Plasmodium falciparum K1 strain is reported. Structurally simplified analogues of antiplasmodial active alkaloids presented similar levels of activity as their corresponding natural products extracted from Guiera senegalensis and Mitragyna inermis with IC values on chloroquine-resistant P. falciparum K1 strain of up to 10. Read More

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http://dx.doi.org/10.1002/ddr.21494DOI Listing
February 2019
2 Reads

Effect of Syringic acid on antioxidant biomarkers and associated inflammatory markers in mice model of asthma.

Drug Dev Res 2019 03 25;80(2):253-261. Epub 2018 Nov 25.

Department of Pediatrics, The First Affiliated Hospital of Nanjing Medical University, Nanjing, Jiangsu, China.

Asthma is termed as the induction of chronic inflammation in the airway lumen of lungs due to accumulation of inflammatory cells which affects normal breathing process. Prolonged accumulation of inflammatory cells leads to oxidative stress and suppression of antioxidant activities. Therefore, in our present investigation, a potential phenolic compound, Syringic acid was tested for the suppression of inflammatory markers toward an antiasthmatic activity in ovalbumin (OVA)-induced asthmatic mice model. Read More

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http://dx.doi.org/10.1002/ddr.21487DOI Listing
March 2019
2 Reads

Synthesis, anticonvulsant screening, and molecular modeling studies of new arylalkylimidazole oxime ether derivatives.

Drug Dev Res 2019 03 25;80(2):269-280. Epub 2018 Nov 25.

Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Hacettepe University, Ankara, Turkey.

In this study, 15 new oxime ether derivatives were synthesized and their anticonvulsant activities were screened in vivo. The compounds were synthesized by the reaction of various alkyl halides with 1-(2-naphthyl)-2-(1H-imidazol-1-yl)ethanone oxime. Their anticonvulsant activities were determined using acute (maximal electroshock, subcutaneous metrazol [SCM], and 6 Hz seizure test) and chronic (corneal-kindled mouse) seizure models, their neurotoxic effects were evaluated by models of behavioral toxicity according to the Epilepsy Therapy Screening Program protocol of the NIH. Read More

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http://dx.doi.org/10.1002/ddr.21491DOI Listing
March 2019
17 Reads

Microsponge: An emerging drug delivery strategy.

Drug Dev Res 2019 03 19;80(2):200-208. Epub 2018 Nov 19.

Department of Pharmacology, School of pharmaceutical Sciences, Jaipur National University, Jaipur, Rajasthan, India.

Microsponges are the spherical particles ranging from 5 to 300 μm in size. These are further made up of clusters of smaller spheres. They are designed for delivering the drug efficiently at a comparatively lesser dose and enhancing the stability, modifying the drug release profile and minimizing the side effects. Read More

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http://dx.doi.org/10.1002/ddr.21492DOI Listing
March 2019
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Drug sales confirm clinical advantage of multi-target inhibition of drug escapes by anticancer kinase inhibitors.

Drug Dev Res 2019 03 13;80(2):246-252. Epub 2018 Nov 13.

Bioinformatics and Drug Design Group, Department of Pharmacy, National University of Singapore, Singapore, Singapore.

The clinical advantage of co-targeting cancer drug escape has been indicated by the percentage of these co-targeting drugs among all multi-target drugs in clinics and clinical trials. This clinical advantage needs to be further interrogated from such perspectives as the clinical impact of multi-target inhibition of drug-escape mediators. This impact may be reflected by drug sales data, that is, multi-target inhibition of higher number of drug-escape mediators favors the expanded coverage of drug-resistant patients leading to higher sales. Read More

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http://doi.wiley.com/10.1002/ddr.21486
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http://dx.doi.org/10.1002/ddr.21486DOI Listing
March 2019
24 Reads

Preparation, optimization, and pharmacokinetic study of nanoliposomes loaded with triacylglycerol-bound punicic acid for increased antihepatotoxic activity.

Drug Dev Res 2019 03 10;80(2):230-245. Epub 2018 Nov 10.

Department of Pharmaceutics and Tissue Engineering, School of Pharmacy, Jiangsu University, Zhenjiang, P.R. China.

Punicic acid of pomegranate oil (PAP) has gained heightened interest due to several health benefits, such as anticarcinogenic, antidiabetic, and antiatherosclerotic properties. However, these bioactivities have been hampered by chemical instability, poor water solubility, rapid metabolism, and low bioavailability of PAP. Therefore, this study was aimed at optimizing the liposomal formulation of Triacylglycerol-bound punicic acid with its regioisomers (TPAR) for improved oral bioavailability and increased hepatoprotection through antioxidation and anti-inflammation. Read More

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http://doi.wiley.com/10.1002/ddr.21485
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http://dx.doi.org/10.1002/ddr.21485DOI Listing
March 2019
28 Reads
0.734 Impact Factor

Functional mechanism of tracheal relaxation, antiasthmatic, and toxicological studies of 6-hydroxyflavone.

Drug Dev Res 2019 03 5;80(2):218-229. Epub 2018 Nov 5.

Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, Mexico.

Previously, we described tracheal rat rings relaxation by several flavonoids, being 6-hydroxyflavone (6-HOF) the most active derivative of the series. Thus, its mechanism of action was determined in an ex vivo tracheal rat ring bioassay. The anti-asthmatic effect was assayed in in vivo OVAlbumin (OVA)-sensitized guinea pigs. Read More

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http://doi.wiley.com/10.1002/ddr.21484
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http://dx.doi.org/10.1002/ddr.21484DOI Listing
March 2019
23 Reads
0.734 Impact Factor

Silver carbene complexes: An emerging class of anticancer agents.

Drug Dev Res 2019 03 1;80(2):188-199. Epub 2018 Nov 1.

University of Kansas Medical Center, Kansas City, Kansas.

Cancer is a major global health problem with large therapeutic challenges. Although substantial progress has been made in cancer therapy, there still remains a need to develop novel and effective treatment strategies to treat several relapsed and refractory cancers. Recently, there has been growing demand for considering organometallics as antineoplastic agents. Read More

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http://doi.wiley.com/10.1002/ddr.21478
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http://dx.doi.org/10.1002/ddr.21478DOI Listing
March 2019
4 Reads

Design, synthesis, and biological evaluation of Helicobacter pylori inosine 5'-monophosphate dehydrogenase (HpIMPDH) inhibitors.

Drug Dev Res 2019 02 1;80(1):125-132. Epub 2018 Nov 1.

Department of Pharmaceutical Chemistry, Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM's NMIMS, Mumbai, India.

Inosine 5'-monophosphate dehydrogenase (IMPDH) catalyzes a crucial step in the biosynthesis of guanine nucleotides. Being a validated target for immunosuppressive, antiviral, and anticancer drug development, lately it has been exploited as a promising target for antimicrobial therapy. Extending our previous work on Mycobacterium tuberculosis IMPDH, GuaB2, inhibitor development, we screened a set of 23 new chemical entities (NCEs) with substituted flavone (Series 1) and 1,2,3-triazole (Series 2) core structures for their in vitro Helicobacter pylori IMPDH (HpIMPDH) and human IMPDH2 (hIMPDH2) inhibitory activities. Read More

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http://dx.doi.org/10.1002/ddr.21467DOI Listing
February 2019
10 Reads