53,267 results match your criteria drugs medicinal

Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.

Bioorg Med Chem 2021 May 5;40:116195. Epub 2021 May 5.

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, Ji'nan 250012, China; China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province, 44 West Culture Road, 250012 Jinan, Shandong, PR China. Electronic address:

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are widely used in combination therapies against HIV-1. As a continuation of our efforts to discover and develop "me-better" drugs of DAPYs, novel diarylpyrimidine derivatives were designed, synthesized and evaluated for their anti-HIV activities in MT-4 cells. All the compounds demonstrated strong inhibition activity against wide-type HIV-1 strain (III) with EC values in the range of 2. Read More

View Article and Full-Text PDF

Mechanism-Guided Development of Transition-Metal-Catalyzed C-N Bond-Forming Reactions Using Dioxazolones as the Versatile Amidating Source.

Acc Chem Res 2021 May 12. Epub 2021 May 12.

Center for Catalytic Hydrocarbon Functionalizations, Institute for Basic Science (IBS), Daejeon 34141, Korea.

ConspectusCatalytic reactions that construct carbon-nitrogen bonds are one of central themes in both synthetic and medicinal chemistry since the obtainable nitrogen-containing motifs are commonly encountered in natural products and have also seen a growing prominence as key structural features in marketed drugs and preclinical candidates. Pd-catalyzed cross-couplings, such as Buchwald-Hartwig amination, are at the forefront of such synthetic methods in practical settings. However, they require prefunctionalized substrates such as (hetero)aryl halides that must be prepared independently, often by multiple operations. Read More

View Article and Full-Text PDF

Structural recognition of the MYC promoter G-quadruplex by a quinoline derivative: insights into molecular targeting of parallel G-quadruplexes.

Nucleic Acids Res 2021 May 12. Epub 2021 May 12.

Purdue University, College of Pharmacy, Medicinal Chemistry and Molecular Pharmacology, 575 W Stadium Ave., West Lafayette, IN 47907, USA.

DNA G-Quadruplexes (G4s) formed in oncogene promoters regulate transcription. The oncogene MYC promoter G4 (MycG4) is the most prevalent G4 in human cancers. However, the most studied MycG4 sequence bears a mutated 3'-residue crucial for ligand recognition. Read More

View Article and Full-Text PDF

S-SIL of PCSK9-Active Oligonucleotide as Tools for Accurate Quantification by Mass Spectrometry.

Nucleic Acid Ther 2021 May 11. Epub 2021 May 11.

Oligonucleotide Discovery, Discovery Sciences, BioPharmaceuticals R&D, AstraZeneca, Gothenburg, Sweden.

Stable isotope labeling (SIL) of active pharmaceutical ingredients (API) is a well-established technique for the accurate quantification of small-molecule drugs. As the scope of active ingredients is expanding into areas of larger molecules, such as oligonucleotides (ONs), the development of new quantification techniques is critical. Herein, we describe the analysis of a S-SIL anti-PCSK9 gapmer-type antisense ON. Read More

View Article and Full-Text PDF

Potential beneficial effects of kefir and its postbiotic, kefiran, on child food allergy.

Food Funct 2021 May;12(9):3770-3786

Laboratory of Pharmaceutical and Medicinal Chemistry (PharMedChem), Federal University of Amapá, Macapá, Brazil.

Food allergies are known as the public health problem, affecting people of all age groups, but more commonly in babies and children, with consequences for nutritional status and quality of life. The increase in the consumption of healthy foods has consequently led to an increased demand for functional foods with specific health benefits. Thus, the pharmaceutical industry's interest in natural products has grown every time and is therefore considered as an alternative to synthetic drugs. Read More

View Article and Full-Text PDF

Utilizing Xenogeneic Cells As a Therapeutic Agent for Treating Diseases.

Cell Transplant 2021 Jan-Dec;30:9636897211011995

Sex Hormone Research Center, Department of Medical Laboratory Science and Biotechnology, China Medical University and Hospital, Taichung, Taiwan.

The utilization of biologically produced cells to treat diseases is a revolutionary invention in modern medicine after chemically synthesized small molecule drugs and biochemically made protein drugs. Cells are basic units of life with diverse functions in mature and developing organs, which biological properties could be utilized as a promising therapeutic approach for currently intractable and incurable diseases. Xenogeneic cell therapy utilizing animal cells other than human for medicinal purpose has been studied as a new way of treating diseases. Read More

View Article and Full-Text PDF

Integrated gut microbiota and fecal metabolomics reveal the renoprotective effect of Rehmanniae Radix Preparata and Corni Fructus on adenine-induced CKD rats.

J Chromatogr B Analyt Technol Biomed Life Sci 2021 Apr 24;1174:122728. Epub 2021 Apr 24.

Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, PR China. Electronic address:

Rehmanniae Radix Preparata (RR) and Corni Fructus (CF), well-known traditional Chinese medicines (TCMs), were generally used together in the clinical practices to treat chronic kidney disease (CKD) with synergistic effects for thousands of years, but their combination mechanism remains largely unknown so far. Recent evidences have implicated intestinal flora as potential targets for the therapy of CKD. In this study, the CKD rat model was induced by adenine. Read More

View Article and Full-Text PDF

An overview on the role of plant-derived tannins for the treatment of lung cancer.

Phytochemistry 2021 May 8;188:112799. Epub 2021 May 8.

Department of Biochemistry, ICMR-National Institute for Research in Environmental Health, Bhopal, Madhya Pradesh, India. Electronic address:

Lung cancer is the leading cause of cancer-related death globally. Despite many advanced approaches to treat cancer, they are often ineffective due to resistance to classical anti-cancer drugs and distant metastases. Currently, alternative medicinal agents derived from plants are the major interest due to high bioavailability and fewer adverse effects. Read More

View Article and Full-Text PDF

The selective 5-HT receptor biased agonists, F15599 and F13714, show antidepressant-like properties after a single administration in the mouse model of unpredictable chronic mild stress.

Psychopharmacology (Berl) 2021 May 10. Epub 2021 May 10.

Department of Pharmacodynamics, Faculty of Pharmacy, Jagiellonian University Medical College, Krakow, Poland.

Rationale: The prevalence of depression is ever-increasing throughout the population. However, available treatments are ineffective in around one-third of patients and there is a need for more effective and safer drugs.

Objectives: The antidepressant-like and procognitive effects of the "biased agonists" F15599 (also known as NLX-101) which preferentially targets postsynaptic 5-HT receptors and F13714, which targets 5-HT autoreceptors, were investigated in mice. Read More

View Article and Full-Text PDF

From Precision Metapharmacology to Patient Empowerment: Delivery of Self-Care Practices for Epilepsy, Pain, Depression and Cancer Using Digital Health Technologies.

Front Pharmacol 2021 23;12:612602. Epub 2021 Apr 23.

Department of Pharmacotherapy, Skaggs Pharmacy Institute, University of Utah, Salt Lake City, UT, United States.

To improve long-term outcomes of therapies for chronic diseases, health promotion and lifestyle modifications are the most promising and sustainable strategies. In addition, advances in digital technologies provide new opportunities to address limitations of drug-based treatments, such as medication non-adherence, adverse effects, toxicity, drug resistance, drug shortages, affordability, and accessibility. Pharmaceutical drugs and biologics can be combined with digital health technologies, including mobile medical apps (digital therapeutics), which offer additional clinical benefits and cost-effectiveness. Read More

View Article and Full-Text PDF

Characterization of pharmaco-EEG fingerprint and sleep-wake profiles of Lavandula angustifolia Mill. essential oil inhalation and diazepam administration in rats.

J Ethnopharmacol 2021 May 7:114193. Epub 2021 May 7.

Division of Biological Science, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla 90110, Thailand; Biosignal Research Center for Health, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla, 90110, Thailand. Electronic address:

Ethnopharmacological Relevance: Lavandula angustifolia Mill. essential oil (Lavender EO) has a long history of medicinal use and is particularly claimed to possess anxiolytic and sedative properties. Lavender EO aromatherapy has been used to reduce distress and improve insomnia naturally. Read More

View Article and Full-Text PDF

Design, synthesis, structural and molecular characterization, toxicity, psychotropic activity and molecular docking evaluation of a novel phenytoin derivative: 3-decyl-5,5-diphenylimidazolidine-2,4-dione.

J Biomol Struct Dyn 2021 May 10:1-18. Epub 2021 May 10.

Laboratory of Medicinal Chemistry, Drug Sciences Research Center, Faculty of Medicine and Pharmacy, Mohammed V University in Rabat, Rabat, Morocco.

The hydantoin scaffold is of substantial importance and it is commonly used in drug discovery. Herein, we report the synthesis of a novel phenytoine (a hydantoin derivative) with high yield by the reaction of phenytoin with 1-bromodecyl agent. Namely, 3-decyl-5,5- diphenylimidazolidine-2,4-dione (3DDID). Read More

View Article and Full-Text PDF

Fabrication of versatile targeted lipopolymersomes for improved camptothecin efficacy against colon adenocarcinoma and .

Expert Opin Drug Deliv 2021 May 10. Epub 2021 May 10.

Pharmaceutical Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.

: Hybrid vesicular systems (lipopolymersomes) are promising platforms for minimizing the liposomes and polymersomes disadvantages in terms of chemotherapeutic transportation. In this regard, lipopolymersome has been designed to integrate the advantage of both polymersomes and liposomes to enable better structural integrity of the bilayer after encapsulation of hydrophobic drugs while maintaining the soft nature of liposomes, superior serum stability, and high encapsulation efficiency of cargos in the bilayer segment.: In the present study, we reported preparation and characterization of five camptothecin (CPT)-loaded lipopolymersomal formulations composed of poly (ethylene glycol)-poly (lactic acid) (PEG-PLA) and dipalmitoylphosphatidylcholine (DPPC) at different molar ratios using film rehydration method. Read More

View Article and Full-Text PDF

Kinase Inhibitors as Underexplored Antiviral Agents.

J Med Chem 2021 May 10. Epub 2021 May 10.

Centro de Investigaciones Biológicas Margarita Salas (CSIC), Ramiro de Maeztu 9, 28040 Madrid, Spain.

Viral infections are a major health problem; therefore, there is an urgent need for novel therapeutic strategies. Antivirals used to target proteins encoded by the viral genome usually enhance drug resistance generated by the virus. A potential solution may be drugs acting at host-based targets since viruses are dependent on numerous cellular proteins and phosphorylation events that are crucial during their life cycle. Read More

View Article and Full-Text PDF

Safe Polycationic Dendrimers as Potent Oral In Vivo Inhibitors of : A New Therapy to Take Down Tuberculosis.

Biomacromolecules 2021 May 10. Epub 2021 May 10.

Laboratoire de Chimie de Coordination du CNRS, 205 Route de Narbonne, BP 44099, 31077 Toulouse Cedex 4, France.

The long-term treatment of tuberculosis (TB) sometimes leads to nonadherence to treatment, resulting in multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis. Inadequate bioavailability of the drug is the main factor for therapeutic failure, which leads to the development of drug-resistant cases. Therefore, there is an urgent need to design and develop novel antimycobacterial agents minimizing the period of treatment and reducing the propagation of resistance at the same time. Read More

View Article and Full-Text PDF

SUMOylation Wrestles With the Occurrence and Development of Breast Cancer.

Front Oncol 2021 21;11:659661. Epub 2021 Apr 21.

Key Laboratory of the Ministry of Education for Medicinal Resources and Natural Pharmaceutical Chemistry, National Engineering Laboratory for Resource Developing of Endangered Chinese Crude Drugs in Northwest of China, College of Life Sciences, Shaanxi Normal University, Xi'an, China.

Breast cancer has the highest incidence among cancers and is the most frequent cause of death in women worldwide. The detailed mechanism of the pathogenesis of breast cancer has not been fully elucidated, and there remains a lack of effective treatment methods for the disease. SUMOylation covalently conjugates a large amount of cellular proteins, and affects their cellular localization and biological activity to participate in numerous cellular processes. Read More

View Article and Full-Text PDF

Hypnotic Effect of . Hydroalcoholic Extract in Pentobarbital-Treated Mice.

Neurol Res Int 2021 21;2021:5521019. Epub 2021 Apr 21.

Neuroscience Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.

Background: Current drugs used in the management of insomnia are associated with side effects. The use of medicinal herbs for insomnia treatment has recently been suggested.

Objective: The present study aimed to determine the hypnotic activity of the hydroalcoholic extract of . Read More

View Article and Full-Text PDF

Therapeutic Potential of Bioactive Compounds in Honey for Treating Osteoarthritis.

Front Pharmacol 2021 21;12:642836. Epub 2021 Apr 21.

Facultad de Ciencias de La Salud, Universidad Anáhuac México Sur, Ciudad de México, Mexico.

Dysregulation of joint tissue homeostasis induces articular degenerative changes and musculoskeletal diseases such as osteoarthritis. This pathology represents the first cause of motor disability in individuals over 60 years of age, impacting their quality of life and the costs of health systems. Nowadays, pharmacological treatments for cartilage disease have failed to achieve full tissue regeneration, resulting in a functional loss of the joint; therefore, joint arthroplasty is the gold standard procedure to cure this pathology in severe cases of Osteoarthritis. Read More

View Article and Full-Text PDF

The burden of cannabis-attributed pediatric and adult emergency department visits.

Acad Emerg Med 2021 May 9. Epub 2021 May 9.

Oregon Health and Science University, Department of Emergency Medicine, Center for Policy and Research in Emergency Medicine, Portland, Oregon, United States.

States that have legalized cannabis for medicinal or retail use have noted increases in emergency department (ED) visits associated with cannabis-associated harms. However, most studies are retrospective and identify cannabis-related visits using diagnosis codes or THC-positive urine drug immunoassays. These identification methods are limited. Read More

View Article and Full-Text PDF

Potential new targets and drugs related to histone modifications in glioma treatment.

Bioorg Chem 2021 Apr 24;112:104942. Epub 2021 Apr 24.

Graduate School, Shandong First Medical University & Shandong Academy of Medical Sciences, Taian, Shandong, China; Department of Neurology, Linyi People's Hospital, Shandong University, Linyi, Shandong, China; Central Laboratory, Linyi People's Hospital, Shandong University, Linyi, Shandong, China; Key Laboratory of Neurophysiology, Key Laboratory of Tumor Biology, Linyi, Shandong, China. Electronic address:

Glioma accounts for 40-50% of craniocerebral tumors, whose outcome rarely improves after standard treatment. The development of new therapeutic targets for glioma treatment has important clinical significance. With the deepening of research on gliomas, recent researchers have found that the occurrence and development of gliomas is closely associated with histone modifications, including methylation, acetylation, phosphorylation, and ubiquitination. Read More

View Article and Full-Text PDF

An atomic perspective on improving daptomycin's activity.

Biochim Biophys Acta Gen Subj 2021 May 6:129918. Epub 2021 May 6.

Department of Chemistry, State Key Lab of Synthetic Chemistry, The University of Hong Kong, Pokfulam Road, Hong Kong; Laboratory for Marine Drugs and Bioproducts, Qingdao National Laboratory for Marine Science and Technology, Qingdao, PR China. Electronic address:

Background: Recently, through comprehensive medicinal chemistry efforts, we have found a new daptomycin analogue, termed kynomycin, showing enhanced activity against both methicillin-resistant S. aureus and vancomycin-resistant Enterococcus in vitro and in vivo, with improved pharmacokinetics and lower cytotoxicity than daptomycin.

Methods: In this study we compared the physicochemical properties of kynomycin with those of daptomycin from an atomic perspective by using Nuclear Magnetic Resonance spectroscopy and Molecular Dynamics simulations. Read More

View Article and Full-Text PDF

A Novel Dual Agonist of Glucagon-like Peptide-1 Receptors and Neuropeptide Y2 Receptors Attenuates Fentanyl Taking and Seeking in Male Rats.

Neuropharmacology 2021 May 6:108599. Epub 2021 May 6.

Department of Biobehavioral Health Sciences, School of Nursing, University of Pennsylvania, Philadelphia, PA 19104, USA; Department of Psychiatry, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA. Electronic address:

There has been a dramatic increase in illicit fentanyl use in the United States over the last decade. In 2018, more than 31,000 overdose deaths involved fentanyl or fentanyl analogues, highlighting an urgent need to identify effective treatments for fentanyl use disorder. An emerging literature shows that glucagon-like peptide-1 receptor (GLP-1R) agonists attenuate the reinforcing efficacy of drugs of abuse. Read More

View Article and Full-Text PDF

Lipase immobilization on magnetic cellulose microspheres for rapid screening inhibitors from traditional herbal medicines.

Talanta 2021 Aug 30;231:122374. Epub 2021 Mar 30.

CAS Key Laboratory of Chemistry of Northwestern Plant Resources, Key Laboratory for Natural Medicines of Gansu Province, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences (CAS), Lanzhou, 730000, PR China. Electronic address:

With a dramatic increase in the incidence of obesity, it is significant to screen lipase inhibitors from traditional herbal medicines as drugs to treat obesity. Lipase inhibitors currently used to treat obesity possess the defects of toxicity and off-target effects. Thus, there is an urgent need to explore more safe, effective and targeted anti-obesity drugs from traditional herbal medicines. Read More

View Article and Full-Text PDF

Experimental design optimization of simultaneous enantiomeric separation of atenolol and chlorthalidone binary mixture by high-performance liquid chromatography using polysaccharide-based stationary phases.

Chirality 2021 May 8. Epub 2021 May 8.

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

In this work, enantiomeric separation of a drug combination of two chiral drugs, namely, atenolol and chlorthalidone, is described. Prior investigation of the effect of different variables on the resolution of the enantiomers' peaks and the total run time represented by the retention time of the last eluted peak was conducted using face-centered composite design. Twenty-two experiments were carried out by varying the chiral stationary phase type as a categorical factor and mobile phase composition including the percentage of ethanol and percentage of diethylamine as continuous factors. Read More

View Article and Full-Text PDF

Chemical profiling, in vitro antioxidant, membrane stabilizing and antimicrobial properties of wild growing Murraya paniculata from Amarkantak (M.P.).

Sci Rep 2021 May 7;11(1):9691. Epub 2021 May 7.

Department of Biotechnology, Indira Gandhi National Tribal University, Amarkantak, Anuppur, Madhya Pradesh, 484887, India.

The excessive usage of antibiotics in humans and veterinary medicine has lead to the emergence of antibiotic resistance and now requires the use of novel antibiotics. There has been increased interest towards plants as source of drugs because of their pharmacological potency and long traditional usage. The aim of the current study was to evaluate bioactive components, antioxidant, and anti-inflammatory activities of the leaf extracts of Murraya paniculata, a plant traditionally used in Indian medicinal system. Read More

View Article and Full-Text PDF

Complications associated with intrathecal drug delivery in a paediatric patient with Niemann-Pick type C.

BMJ Case Rep 2021 May 7;14(5). Epub 2021 May 7.

Neurosurgery, Great Ormond Street Hospital for Children, London, UK.

We report on a male subject with a diagnosis of Niemann-Pick type C (NPC). He received an experimental medicinal product intrathecally initially via lumbar puncture (LP) and eventually via intrathecal drug delivery device. Shortly after implantation, the device catheter migrated outside of the intrathecal space and coiled subcutaneously. Read More

View Article and Full-Text PDF

In silico and in vitro screening of licensed antimalarial drugs for repurposing as inhibitors of hepatitis E virus.

In Silico Pharmacol 2021 4;9(1):35. Epub 2021 May 4.

Laboratory of Pharmacology and Toxicology, Department of Biochemistry, Faculty ofScience, University of Yaounde I, P.O. Box 812, Yaounde, Cameroon.

Abstract: Hepatitis E virus (HEV) infection is emerging in Cameroon and represents one of the most common causes of acute hepatitis and jaundice. Moreover, earlier reports showed evidence of falciparum malaria/HEVcoexistence. Although the Sofosbuvir/Ribavirin combination was recently proposed in the treatment of HEV-infected patients, no specific antiviral drug has been approved so far, thereby urging the search for new therapies. Read More

View Article and Full-Text PDF

Machine learning techniques applied to the drug design and discovery of new antivirals: a brief look over the past decade.

Expert Opin Drug Discov 2021 May 7:1-15. Epub 2021 May 7.

Escola de Artes, Ciências e Humanidades, Universidade de São Paulo (USP), São Paulo, Brazil.

: Drug design and discovery of new antivirals will always be extremely important in medicinal chemistry, taking into account known and new viral diseases that are yet to come. Although machine learning (ML) have shown to improve predictions on the biological potential of chemicals and accelerate the discovery of drugs over the past decade, new methods and their combinations have improved their performance and established promising perspectives regarding ML in the search for new antivirals.: The authors consider some interesting areas that deal with different ML techniques applied to antivirals. Read More

View Article and Full-Text PDF

A computational study of structural differences of binding of NADP and G6P substrates to G6PD Mediterranean, G6PD A-, G6PD Cairo and G6PD Gaza mutations.

Blood Cells Mol Dis 2021 Apr 27;89:102572. Epub 2021 Apr 27.

Division of Hematology, Department of Internal Medicine, University of Utah School of Medicine, Salt Lake City, UT, United States of America. Electronic address:

Glucose-6-phosphate dehydrogenase (G6PD) deficiency is a common X-linked inherited enzymopathic disorder that may lead to transfusion-requiring acute hemolytic anemia (AHA) triggered by fava beans ingestion, infection or some drugs. The gene encoding for G6PD carries a large number of genetic variants that have varying pathogenicity. We reported on three G6PD variants in the Gaza Strip Palestinian population with differing clinical impacts and frequencies: G6PD Mediterranean, African G6PD A-, and G6PD Cairo. Read More

View Article and Full-Text PDF

In silico network pharmacology and in vivo analysis of berberine-related mechanisms against type 2 diabetes mellitus and its complications.

J Ethnopharmacol 2021 May 3;276:114180. Epub 2021 May 3.

Endocrinology Department, Affiliated Hospital to Changchun University of Chinese Medicine, Changchun, Jilin, China. Electronic address:

Ethnopharmacological Relevance: Berberine (BBR), extracted from the traditional medicinal plant Coptis chinensis Franch., has been widely used for the treatment of type 2 diabetes mellitus (T2DM) and its complications.

Aim Of The Study: To determine the potential pharmacological mechanisms underlying BBR therapeutic effect on T2DM and its complications by in silico network pharmacology and experimental in vivo validation. Read More

View Article and Full-Text PDF