303 results match your criteria Central Nervous System Agents in Medicinal Chemistry[Journal]


Drug Repositioning: Antimalarial Activities of GABA Analogs in Mice Infected with Plasmodium berghei.

Cent Nerv Syst Agents Med Chem 2020 Jun 4. Epub 2020 Jun 4.

Department of Medical Microbiology & Parasitology, College of Health Sciences, Ladoke Akintola University of Technology, Ogbomoso, Oyo State. Nigeria.

Background: Drug repositioning is becoming popular due to the development of resistance to almost all the recommended antimalarials. Pregabalin and gabapentin are chemical analogs of gamma-aminobutyric acid (GABA) approved for the treatment of epilepsy and neuropathic pain.

Objective: This study investigates acute toxicities and antimalarial activities of pregabalin and gabapentin in the murine malarial model. Read More

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http://dx.doi.org/10.2174/1871524920666200604151907DOI Listing

α-Substituted Lactams and Acetamides: Ion Channel Modulators that show Promise in Treating Drug-resistant Epilepsy.

Cent Nerv Syst Agents Med Chem 2020 May 9. Epub 2020 May 9.

Chemistry Program, University of Houston - Clear Lake, Houston, TX 77058. United States.

The two main problems in the pharmacotherapy of epilepsy are resistance to currently available first-line medications (which occurs in about one third of patients) and the high incidence of side effects. To address these two challenges, extensive efforts are being undertaken to design new, structurally distinct antiepileptic drugs with a broad spectrum of anticonvulsant activity. Tests in animal models of epilepsy indicate that α-substituted lactams and acetamides show a broad spectrum of anticonvulsant activity (including very promising activity in drug-resistant models) as well as an excellent safety profile. Read More

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http://dx.doi.org/10.2174/1871524920666200510005458DOI Listing

Behavioral Evaluation for Aqueous and Ethanol Extracts of Suaeda vermiculata Forssk.

Cent Nerv Syst Agents Med Chem 2020 Mar 19. Epub 2020 Mar 19.

Medicinal Chemistry and Pharmacognosy Department, Qassim University, College of Pharmacy, Qassim. Saudi Arabia.

Background: Suaeda vermiculata is one of the widely distributed halophytes in central Saudi Arabia. The plant is used as a remedy for liver diseases, jaundice, and inflammation. S. Read More

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http://dx.doi.org/10.2174/1871524920666200319142536DOI Listing

Potential mechanisms involved in the anticonvulsant effect of methanol extract of Pyrenancantha staudtii in mice.

Cent Nerv Syst Agents Med Chem 2020 02 10. Epub 2020 Feb 10.

Department of Microbiology and Parasitology, Ladoke Akintola University of Technology Ogbomoso, Nigeria.

Objective: To determine the potential effect of Pyrenancantha staudtii extract on experimentally induced seizures in mice and to evaluate the role of benzodiazepines, naloxone, and serotonin within these pathways.

Methods: Animals behaviours were evaluated using open field, hexobarbitone-induced sleep model, and anticonvulsant activity using picrotocin-, or strychnine-, or isoniazid-induced convulsions. To understand the mode of action of the anticonvulsant activity of the plant, three notable antagonists (flumazenil, 3 mg/kg; naloxone 5 mg/kg, i. Read More

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http://dx.doi.org/10.2174/1871524920666200211113633DOI Listing
February 2020

Theoretical Study of Monoamine Oxidase B Inhibitors as Drug Candidates for Treatment of Parkinson's Disease.

Cent Nerv Syst Agents Med Chem 2020 02 16. Epub 2020 Feb 16.

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

Background: Drugs used for Parkinson's disease (PD) are based only on relieving main symptoms, but may present several side effects that are typical of such pharmacological treatment.

Methods: This study aimed to use in silico methods for drug designing inhibitors of PD therapeutic target monoamine oxidase B (MAO-B). Thus, 20 MAO-B inhibitors from BindingDB database were selected, then it was performed a calculation of their descriptors at DFT B3LYP/6-31G** level of theory. Read More

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http://dx.doi.org/10.2174/1871524920666200217110211DOI Listing
February 2020

A link between brain insulin resistance and cognitive dysfunctions: targeting Ca2+/cAMP signalling.

Cent Nerv Syst Agents Med Chem 2020 Jan 29. Epub 2020 Jan 29.

Department of Pharmacology - Escola Paulista de Medicina - Universidade Federal de São Paulo -- Tel.: 55 11 5576-4973, Rua Pedro de Toledo, 669 - Vila Clementino, São Paulo - SP. Brazil.

Background: A Correlation Between Cognitive Dysfunctions And Brain Insulin Resistance Has Been Established By Several Clinical And Experimental Studies. Consistent Data Support That People Diagnosed With Brain Insulin Resistance, Resulted From Diabetes, Have Shown An Increased Risk Of Presenting Cognitive Dysfunctions, Clinical Signs Of Dementia And Depression, Then Speculating A Role Of Dysregulations Related To Insulin Signalling In These Diseases. Furthermore, It Is Currently Extremely Discussed That Ca Signalling, And Its Dysregulations, May Be A Factor Which Could Correlate Brain Insulin Resistance And Cognitive Dysfunctions. Read More

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http://dx.doi.org/10.2174/1871524920666200129121232DOI Listing
January 2020

An Evaluation of the Effects of Pyridoxal Phosphate in Chlorpromazineinduced Parkinsonism using Mice.

Cent Nerv Syst Agents Med Chem 2020 ;20(1):13-25

Behavioural Neuroscience/Neuropharmacology Unit, Department of Pharmacology, Ladoke Akintola University of Technology, Osogbo, Osun State, Nigeria.

Background: Parkinsonism is a neurodegenerative disorder with a heavy disease burden, despite the discovery and application of drugs. Current research is beginning to suggest the possible crucial roles of micronutrients such as pyridoxal phosphate in the prevention or management of neurodegenerative disorders.

Objective: We investigated the possible protective effects of supplemental pyridoxal phosphate in Chlorpromazine (CPZ)-induced Parkinsonism-like changes in mice. Read More

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http://dx.doi.org/10.2174/1871524920666200120142508DOI Listing
January 2020

Electronegativity in Substituted-4(H)-quinazolinones Causes Anxiolysis without a Sedative-hypnotic Adverse Reaction in Female Wistar Rats.

Cent Nerv Syst Agents Med Chem 2020 ;20(1):26-40

Department of Pharmaceutical Sciences, Dr. Harisingh Gour Viswavidyalaya, Sagar, MP, India.

Objective: In the current study, the synthesis, characterization, and neuropharmacology of quinazolinone tethered with aromatic (3a-3i) and heteroaromatic substitution (3j, 3k, and 3l) as effective anxiolytic agents are reported.

Background: Anxiety and depression are often comorbid with neurological as well as other medical maladies. Clinically known anxiolytics (Benzodiazepines) are accompanied by untoward sedation and other CNS depressive actions. Read More

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http://dx.doi.org/10.2174/1871524920666191220112545DOI Listing
January 2020

Screening of Some Novel 4, 5 Disubstituted 1, 2, 4-Triazole-3-thiones for Anticonvulsant Activity.

Cent Nerv Syst Agents Med Chem 2020 ;20(1):41-48

Department of Pharmacy, Ram-Eesh Institute of Vocational & Technical Education, Plot No. 3, Knowledge Park-I, Greater Noida, UP, India.

Objective: In the present study, we synthesized fifteen 4, 5-disubstituted 1, 2, 4-triazol- 3-thione derivatives and evaluated for anticonvulsant activity with neurotoxicity determination.

Methods: The synthesized compounds were characterized using FTIR, 1H-NMR and MS. The molecular docking study was also performed to study the interactions of compounds with LYS329 residue of gamma amino butyric acid aminotransferase (GABA-AT) using Autodock 4. Read More

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http://dx.doi.org/10.2174/1871524919666191209103003DOI Listing
January 2020

Design, Synthesis and Biological Activity of Some 4, 5-Disubstituted-2, 4- Dihydro-3H-1, 2, 4- Triazole-3-Thione Derivatives.

Cent Nerv Syst Agents Med Chem 2019 ;19(3):197-205

Department of Pharmacy, Ram-Eesh Institute of Vocational & Technical Education, Knowledge Park-I, Greater Noida, UP, India.

Background: In the present study, 4, 5-disubstituted triazol-3-thione derivatives were synthesized and evaluated for anticonvulsant activity along with neurotoxicity determination.

Materials And Methods: The synthesized compounds were characterized using FTIR, 1H-NMR and MS. The anticonvulsant activity was assessed by Maximal Electroshock (MES) test and subcutaneous Pentylenetetrazole (scPTZ) tests and neurotoxicity was assessed by rotarod test. Read More

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http://dx.doi.org/10.2174/1871524919666190722144424DOI Listing

Noradrenergic Regulation of Hippocampus-Dependent Memory.

Cent Nerv Syst Agents Med Chem 2019 ;19(3):187-196

Department of Biology, York University, 4700 Keele Street, Toronto, ON, M3J 1P3, Canada.

Neuromodulation regulates critical functions of CNS synapses, ranging from neural circuit development to high-order cognitive processes, including learning and memory. This broad scope of action is generally mediated through alterations of the strength of synaptic transmission (i.e. Read More

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http://dx.doi.org/10.2174/1871524919666190719163632DOI Listing

An Assessment of the Effects of Azodicarbonamide-containing Diet on Neurobehaviour, Brain Antioxidant Status and Membrane Lipid Peroxidation Status in Rats.

Cent Nerv Syst Agents Med Chem 2020 ;20(1):49-57

Department of Pharmacology and Therapeutics, Ladoke Akintola University of Technology, Osogbo, Osun State, Nigeria.

Background: Azodicarbonamide is a dough-enhancer used in the process of breadmaking in countries like Nigeria. While there have been suggestions that it is a sensitizer of the respiratory system, there is a dearth of information on its effects on the central nervous system.

Aim: This study assessed the effects of azodicarbonamide on the central nervous system (ADA) in rats. Read More

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http://dx.doi.org/10.2174/1871524919666191104154009DOI Listing
January 2020

The Computational Analysis Conducted on miRNA Target Sites in Association with SNPs at 3'UTR of ADHD-implicated Genes.

Cent Nerv Syst Agents Med Chem 2020 ;20(1):58-75

Department of Cellular and Molecular Biology, Faculty of Life Sciences and Biotechnology, Shahid Beheshti University G.C., Tehran, Iran.

Background: Attention-deficit/hyperactivity disorder (ADHD) is a frequent chronic neuropsychiatric disorder in which different factors including environmental, genetic, and epigenetic factors play an important role in its pathogenesis. One of the effective epigenetic factors is recognized as MicroRNAs (miRNAs). On the other hand, it has been indicated that the single nucleotide polymorphism (SNPs) present within 3'UTR (3' untranslated region) of mRNAs can influence the regulation of miRNA-mediated gene and susceptibility to a diversity of human diseases. Read More

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http://dx.doi.org/10.2174/1871524919666191014104843DOI Listing
January 2020
4 Reads

A Novel Highly Selective Cannabinoid CB2 Agonist Reduces in vitro Growth and TGF-beta Release of Human Glial Cell Tumors.

Cent Nerv Syst Agents Med Chem 2019 ;19(3):206-214

Department of Medicine, Surgery and Neurosciences, University of Siena, Siena, Italy.

Background: Cannabinoid receptors have been detected in human gliomas and cannabinoids have been proposed as novel drug candidates in the treatment of brain tumors.

Aims: To test the in vitro antitumor activity of COR167, a novel cannabinoid CB2-selective agonist displaying a high binding affinity for human CB2 receptors, on tumor cells isolated from human glioblastoma multiforme and anaplastic astrocytoma.

Methods: Glioma cell cultures were established from two glioblastoma multiforme and two anaplastic astrocytomas. Read More

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http://dx.doi.org/10.2174/1871524919666190923154351DOI Listing
April 2020
1 Read

Berberine: A Plant-derived Alkaloid with Therapeutic Potential to Combat Alzheimer's disease.

Cent Nerv Syst Agents Med Chem 2019 ;19(3):154-170

Department of Pharmaceutics, Amity Institute of Pharmacy, Amity University Uttar Pradesh, Sec 125, Noida, 201303, Uttar Pradesh, India.

Berberine (a protoberberine isoquinoline alkaloid) has shown promising pharmacological activities, including analgesic, anti-inflammatory, anticancer, antidiabetic, anti-hyperlipidemic, cardioprotective, memory enhancement, antidepressant, antioxidant, anti-nociceptive, antimicrobial, anti- HIV and cholesterol-lowering effects. It is used in the treatment of the neurodegenerative disorder. It has strong evidence to serve as a potent phytoconstituent in the treatment of various neurodegenerative disorders such as AD. Read More

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http://dx.doi.org/10.2174/1871524919666190820160053DOI Listing
April 2020
1 Read

The Role of Melanin to Dissociate Oxygen from Water to Treat Retinopathy of Prematurity.

Cent Nerv Syst Agents Med Chem 2019 ;19(3):215-222

I.M. Sechenov First Moscow State Medical University (Sechenov University), Trubetskaya Str., 8, bld. 2, Moscow, 119991, Russian Federation.

Background: Retinopathy of Prematurity (ROP) is a potentially blinding disorder that commonly afflicts premature infants who are born prior to 31weeks of gestation or with a body weight less than 1250 grams (about 2.75 pounds). Another risk factor is excessive oxygen in incubators, which can lead to blindness. Read More

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http://dx.doi.org/10.2174/1871524919666190702164206DOI Listing
April 2020
5 Reads

Evaluation of Selected Natural Compounds as Dual Inhibitors of Catechol-O-Methyltransferase and Monoamine Oxidase.

Cent Nerv Syst Agents Med Chem 2019 ;19(2):133-145

Pharmaceutical Chemistry, School of Pharmacy and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.

Background: The most effective symptomatic treatment of Parkinson's disease remains the metabolic precursor of dopamine, L-dopa. To enhance the efficacy of L-dopa, it is often combined with inhibitors of the enzymes, catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO) B, key metabolic enzymes of L-dopa and dopamine.

Objective: This study attempted to discover compounds that exhibit dual inhibition of COMT and MAO-B among a library of 40 structurally diverse natural compounds. Read More

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http://dx.doi.org/10.2174/1871524919666190619090852DOI Listing
January 2020
1 Read

Chirality of Central Nervous System (CNS) Acting Drugs: A Formidable Therapeutic Hurdle Against CNS Diseases.

Cent Nerv Syst Agents Med Chem 2019 ;19(3):171-179

Department of Veterinary Physiology, Pharmacology and Biochemistry, College of Veterinary Medicine, Federal University of Agriculture, P.M.B. 2373, Makurdi, Benue State, Nigeria.

Background: Over fifty percent of drugs being used clinically are chiral and 90% of them are racemates. Unfortunately, they have both adverse and beneficial effects on body systems.

Methods: Because of the erratic effects of chiral compounds on body functional systems, literature search was carried out with a view to identify CNS chiral drugs, their clinical advantages and disadvantages, unique physicochemical properties and structural modifications into safer drugs. Read More

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http://dx.doi.org/10.2174/1871524919666190624150214DOI Listing
April 2020
7 Reads

Conversion of Benzimidazoles, Imidazothiazoles and Imidazoles into more Potent Central Nervous System Acting Drugs.

Cent Nerv Syst Agents Med Chem 2020 ;20(1):3-12

Department of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Federal University of Agriculture, P.M.B. 2373, Makurdi, Benue State, Nigeria.

Background: Benzimidazole (albendazole), imidazothiazole (levamisole) and imidazole (euconazole) are used in chemotherapy of helminthosis and mycosis respectively, with central nervous system (CNS) side effects. But only a limited number of azole groups are used clinically in the treatment of CNS diseases, which are on increase and could not be cured permanently. Due to increased incidence of more challenging new CNS diseases, there is a need for the synthesis of more potent CNS drugs. Read More

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http://dx.doi.org/10.2174/1871524919666190621160323DOI Listing
January 2020
27 Reads

Chemistry and Effects of Brainstem Acting Drugs.

Cent Nerv Syst Agents Med Chem 2019 ;19(3):180-186

Department of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Federal University of Agriculture, P.M.B. 2373, Makurdi, Benue State, Nigeria.

Background: Brain is the most sensitive organ, whereas brainstem is the most important part of Central Nervous System (CNS). It connects the brain and the spinal cord. However, a myriad of drugs and chemicals affects CNS with severe resultant effects on the brainstem. Read More

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http://dx.doi.org/10.2174/1871524919666190620164355DOI Listing
April 2020
11 Reads

Antioxidant Effect of Flavonoids Present in Euterpe oleracea Martius and Neurodegenerative Diseases: A Literature Review.

Cent Nerv Syst Agents Med Chem 2019 ;19(2):75-99

Laboratory of Pharmaceutical and Medicinal Chemistry (PharMedChem), Federal University of Amapa, Macapa, Brazil.

Introduction: Neurodegenerative diseases (NDDs) are progressive, directly affecting the central nervous system (CNS), the most common and recurrent are Alzheimer's disease (AD) and Parkinson's disease (PD). One factor frequently mentioned in the etiology of NDDs is the generation of free radicals and oxidative stress, producing cellular damages. Studies have shown that the consumption of foods rich in polyphenols, especially those of the flavonoid class, has been related to the low risk in the development of several diseases. Read More

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http://dx.doi.org/10.2174/1871524919666190502105855DOI Listing
January 2020
5 Reads

Aging Affects Nicotinic Acetylcholine Receptors in Brain.

Authors:
Yuri N Utkin

Cent Nerv Syst Agents Med Chem 2019 ;19(2):119-124

Laboratory of Molecular Toxinology, Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry RAS, Moscow, Russian Federation.

Background: Aging is a common and inevitable stage in the life cycle of higher organisms. Different organs, including the central nervous system, are affected by aging in different ways. Many processes are involved in aging, and neurodegeneration is one of the aging processes in which the central nervous system is engaged. Read More

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http://dx.doi.org/10.2174/1871524919666190320102834DOI Listing
January 2020
3 Reads

Pharmacological Approach of Pistacia Vera Fruit to Assess Learning and Memory Potential in Chemically-Induced Memory Impairment in Mice.

Cent Nerv Syst Agents Med Chem 2019 ;19(2):125-132

School of Pharmacy, Babu Banarasi Das University, Babu Banarasi Das City, Faizabad Road, Chinhat, Lucknow- 227105, Uttar Pradesh, India.

Objective: The present study was designed to investigate the potential of Pistacia vera (P. vera) fruits in experimental memory impairments in mice.

Material & Methods: Memory impairment was induced in Swiss Albino mice by scopolamine (0. Read More

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http://dx.doi.org/10.2174/1871524919666190304122927DOI Listing
January 2020
4 Reads

Glacial Acetic Acid Catalyzed Synthesis, Physicochemical and Biological Evaluation of Benzodiazepines as Potent CNS Agents.

Cent Nerv Syst Agents Med Chem 2019 ;19(2):146-151

Faculty of Pharmacy, IFTM University, Moradabad-244001, India.

Background: Approach for green chemistry for chemical synthesis is found to be very efficient as it makes the reaction more easily, less tedious, maximize desired products and minimize by-products.

Materials & Methods: Utilizing this approach 1, 5-benzodiazepines and its derivatives have been synthesized and evaluated for skeletal muscle and antianxiety activity. 1, 5-benzodiazepine derivatives have attracted great attention due to its diversity of pharmacological activities and its application in heterocyclic synthesis and medicines. Read More

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http://dx.doi.org/10.2174/1871524919666190227234238DOI Listing
January 2020
26 Reads

Natural Compounds and Drug Discovery: Can Cnidarian Venom Play a Role?

Cent Nerv Syst Agents Med Chem 2019 ;19(2):114-118

Institute for Glycomics and School of Medical Science, Griffith University, Southport, Queensland, Australia.

Natural compounds extracted from organisms and microorganisms are an important resource for the development of drugs and bioactive molecules. Many such compounds have made valuable contributions in diverse fields such as human health, pharmaceutics and industrial applications. Presently, however, research on investigating natural compounds from marine organisms is scarce. Read More

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http://dx.doi.org/10.2174/1871524919666190227234834DOI Listing
January 2020

Acrylamide Induced Toxicity and the Propensity of Phytochemicals in Amelioration: A Review.

Cent Nerv Syst Agents Med Chem 2019 ;19(2):100-113

Department of Biological Sciences, School of Basic and Applied Sciences, Dayananda Sagar University, Shavige Malleshwara Hills, Kumaraswamy Layout, Bengaluru-560 078, Karnataka, India.

Acrylamide is widely found in baked and fried foods, produced in large amount in industries and is a prime component in toxicity. This review highlights various toxicities that are induced due to acrylamide, its proposed mode of action including oxidative stress cascades and ameliorative mechanisms using phytochemicals. Acrylamide formation, the mechanism of toxicity and the studies on the role of oxidative stress and mitochondrial dysfunctions are elaborated in this paper. Read More

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http://dx.doi.org/10.2174/1871524919666190207160236DOI Listing
January 2020
21 Reads

Unraveling the Structural Requirements of Chalcone Chemistry Towards Monoamine Oxidase Inhibition.

Authors:
Bijo Mathew

Cent Nerv Syst Agents Med Chem 2019;19(1):6-7

Division of Drug Design and Medicinal Chemistry Research Lab, Department of Pharmaceutical Chemistry, Ahalia School of Pharmacy, Palakkad-678557, Kerala, India.

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http://dx.doi.org/10.2174/1871524919666190131160122DOI Listing
November 2019
2 Reads

Supplements Offset Paraquat-Induced Behavioral Phenotype and Brain Oxidative Pathways in Mice.

Cent Nerv Syst Agents Med Chem 2019 ;19(1):57-66

Department of Biochemistry, Council of Scientific & Industrial Research (CSIR)-Central Food Technological Research Institute (CFTRI), Mysore, Karnataka, India.

Background: Parkinson's Disease (PD) is characterized by alterations in cerebellum and basal ganglia functioning with corresponding motor deficits and neuropsychiatric symptoms. Involvement of oxidative dysfunction has been implicated for the progression of PD, and environmental neurotoxin exposure could influence such behavior and psychiatric pathology. Assessing dietary supplementation strategies with naturally occurring phytochemicals to reduce behavioral anomalies associated with neurotoxin exposure would have major clinical importance. Read More

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http://www.eurekaselect.com/169002/article
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http://dx.doi.org/10.2174/1871524919666190115125900DOI Listing
November 2019
15 Reads

Development and Characterization of Nasal Delivery of Selegiline Hydrochloride Loaded Nanolipid Carriers for the Management of Parkinson's Disease.

Cent Nerv Syst Agents Med Chem 2019 ;19(1):46-56

Department of Biotechnology, ISF College of Pharmacy, Moga, 142001, Punjab, India.

Introduction: Parkinson's Disease (PD) is one of the most common age-related neurodegenerative disorders which is marked with the loss of dopaminergic neurons. The present study performed on the nose to brain delivery of selegiline hydrochloride loaded nano lipid carrier, suggests that the nasal route is a good mean of targeting the drug directly into the brain.

Methods And Materials: Nanostructured lipid carriers were prepared by using hot homogenization. Read More

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http://dx.doi.org/10.2174/1871524919666181126124846DOI Listing
November 2019
57 Reads

Design, Synthesis, Anticonvulsant Activity, Preclinical Study and Pharmacokinetic Performance of N-{[3-(4-chlorophenyl)-4-oxo-3, 4-dihydroquinazolin- 2-yl] methyl}, 2-[(2-isopropyl-5-methyl) 1-cyclo Hexylidene] Hydrazinecarboxamide.

Cent Nerv Syst Agents Med Chem 2019 ;19(1):31-45

Moradabad Educational Trust Group of Institutions, Faculty of Pharmacy, Moradabad 244001, Uttar Pradesh, India.

Background: N-{[3-(4-chlorophenyl)-4-oxo-3, 4-dihydroquinazolin-2-yl] methyl}, 2-[(2- isopropyl-5-methyl) 1-cyclohexylidene] hydrazinecarboxamide QS11 was designed by computational study. It possessed essential pharmacophoric features for anticonvulsant activity and showed good docking with iGluRs (Kainate) glutamate receptor.

Methods: QSAR and ADMET screening results suggested that QS11 would possess good potency for anticonvulsant activity. Read More

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http://dx.doi.org/10.2174/1871524919666181122124012DOI Listing
November 2019
25 Reads

Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones.

Cent Nerv Syst Agents Med Chem 2019 ;19(1):67-71

Division of Drug Design and Medicinal Chemistry Research Lab, Department of Pharmaceutical Chemistry, Ahalia School of Pharmacy, Palakkad-678557, Kerala, India.

Background: Dual-acting human monoamine oxidase B (hMAO-B) and cholinesterase (ChE) inhibitors are more effective than the classic one-drug one-target therapy for Alzheimer's disease (AD).

Methods: The ChE inhibitory ability of some halogenated thiophene chalcone-based molecules known to be selective hMAO-B inhibitors was evaluated.

Results: Based on the IC50 values, the selected compounds were found to moderately inhibit ChE, with IC50 values in the range of 14-70 µM. Read More

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http://dx.doi.org/10.2174/1871524918666181119114016DOI Listing
November 2019
33 Reads

A Novel Non-invasive Effective Method for Potential Treatment of Degenerative Disc Disease: A Hypothesis.

Cent Nerv Syst Agents Med Chem 2019 ;19(1):8-14

Institute of Physiologically Active Compounds, Russian Academy of Sciences, Chernogolovka, 142432, Russian Federation.

The pathophysiology of the intervertebral discs plays a significant role in the people's life quality. There is not adequate research done in the pathogenesis and treatment of intervertebral disc degeneration. Alternately, self-educated physiology offers a novel and noninvasive method to reverse the degenerated discs. Read More

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http://dx.doi.org/10.2174/1871524918666181017152053DOI Listing
November 2019
39 Reads

Computational Study on the Role of γ-Synuclein in Inhibiting the α-Synuclein Aggregation.

Cent Nerv Syst Agents Med Chem 2019 ;19(1):24-30

Molecular Modelling and Simulation Laboratory, Department of Molecular Biology and Biotechnology, Tezpur University, Tezpur, Assam, India.

Background: α-Synuclein (αS) is the precursor protein present in Lewy Bodies that helps in the formation of highly ordered amyloid fibrils that is associated with the occurrence of Parkinson's disease, a neuro-degenerative disorder. Many reports have now been focused on finding the probable targets to weaken this debilitating disease. Recently γ-synuclein (γS), a presynaptic protein, was highlighted to inhibit the aggregation propensity of αS both in vivo and in vitro. Read More

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http://www.eurekaselect.com/166215/article
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http://dx.doi.org/10.2174/1871524918666181012160439DOI Listing
November 2019
3 Reads

Recent Finding in Repair of the Peripheral Nerve Lesions Using Pharmacological Agents: Common Methods for Evaluating the Repair Process.

Cent Nerv Syst Agents Med Chem 2018 ;18(3):161-172

Department of Medical Physics and Biomedical Engineering, School of Medicine, Tehran University of Medical Science, Tehran, Iran.

Introduction: Peripheral nerve lesion is a common clinical problem that may produce longterm functional defects. Usually, crush injuries, fractures, scars, lacerations, compression, or iatrogenic reasons are reasons for nerve injuries. Unsuccessful treatment of nerve injuries causes partial or total loss of sense, motor, and autonomic functions. Read More

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http://dx.doi.org/10.2174/1871524918666180830101953DOI Listing
January 2018
34 Reads

Classification (Agonist/Antagonist) and Regression "Structure-Activity" Models of Drug Interaction with 5-HT6.

Cent Nerv Syst Agents Med Chem 2018 ;18(3):213-221

Institute of Physiologically Active Compounds, Russian Academy of Sciences, Moscow Region 142432, Chernogolovka, Russian Federation.

Introduction: One promising target for novel psychotropic drugs is the 5-HT6 receptor, GProtein- Coupled Receptor (GPCR) family, displaying seven transmembrane domains. There is considerable interest in how both 5-HT6 receptor agonist and antagonist compounds can have marked procognitive effects.

Methods: An exact structure of the 5-HT6 receptor is not available, so application of powerful methods of (Q)SAR and molecular modelling, which play an essential role in modern drug design, are currently limited to structure-based homology models. Read More

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http://dx.doi.org/10.2174/1871524918666180827100437DOI Listing
January 2018
35 Reads

Brain and Quantum Dots: Benefits of Nanotechnology for Healthy and Diseased Brain.

Authors:
Yuri N Utkin

Cent Nerv Syst Agents Med Chem 2018 ;18(3):193-205

Laboratory of Molecular Toxinology, Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, 117997 Moscow, Russian Federation.

Introduction: The brain is the most complicated organ in a vertebrate's organism. In a human, it contains about two hundred billions of neurons and non-neuronal cells. To understand the mechanisms of the brain functions is the great challenge for the researchers. Read More

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http://dx.doi.org/10.2174/1871524918666180813141512DOI Listing
January 2018
8 Reads

Malaria, Antimalaria Drugs, Drug/Parasite Interactions, and the Brain: A Review of Impacts on Behaviour, Neurochemistry and Structure.

Cent Nerv Syst Agents Med Chem 2018 ;18(3):173-192

Department of Medical Microbiology and Parasitology, Ladoke Akintola University of Technology, Osogbo, Osun State, Nigeria.

Background: Recorded history shows that malaria has plagued mankind for centuries, if not millennia, with the disease infecting and affecting several body tissues, organs and systems; including the central nervous system. Cerebral malaria is a severe form of malaria that may be associated with acute and chronic general behavioural, neurological or neuropsychiatric manifestations. The observation that the use of certain antimalaria drugs may also be associated with behavioural, neurochemical and structural brain changes complicates the picture, as both the infection and its treatment may cause significant changes in brain structure/function and behaviour. Read More

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http://dx.doi.org/10.2174/1871524918666180717111520DOI Listing
January 2018
5 Reads

Neuropharmacological Profile of Gamma-Decanolactone on Chemically-induced Seizure in Mice.

Cent Nerv Syst Agents Med Chem 2018 ;18(3):222-227

Laboratory of Neuropharmacology and Preclinical Toxicology, Postgraduate Program in Biological Sciences: Pharmacology and Therapeutics, Institute of Basic Health Sciences, Federal University of Rio Grande do Sul, Sarmento Leite 500/305, Porto Alegre, RS, CEP 90050-170, Brazil.

Background: Gamma-Decanolactone (GD) is a monoterpene compound that presents anticonvulsant effect in acute and chronic models of epilepsy and it acts as a noncompetitive glutamate antagonist.

Objective: This study evaluated the anticonvulsant profile and the possible mechanism of action of GD in seizures induced by isoniazid (INH; 250 mg/kg), picrotoxin (PCT; 5 mg/kg) and 4- aminopyridine (4-AP; 13 mg/kg) in male mice.

Method: Thirty minutes before the convulsants administration, animals received a single administration of saline, GD (100 or 300 mg/kg) or the positive control diazepam (DZP; 2 mg/kg). Read More

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http://dx.doi.org/10.2174/1871524918666180611103802DOI Listing
January 2018
8 Reads

In-Silico Screening of Ligand Based Pharmacophore, Database Mining and Molecular Docking on 2, 5-Diaminopyrimidines Azapurines as Potential Inhibitors of Glycogen Synthase Kinase-3β.

Cent Nerv Syst Agents Med Chem 2018 ;18(2):150-158

Department of Pharmacy, Banasthali University, Banasthali, Rajasthan 304022, India.

Background: Glycogen synthase kinase-3β plays a significant role in the regulation of various pathological pathways relating to the Central Nervous System (CNS). Dysregulation of Glycogen synthase kinase 3 (GSK-3) activity gives rise to numerous neuroinflammation and neurodegenerative related disorders that affect the whole central nervous system.

Objective: By the sequential application of in-silico tools, efforts have been attempted to design the novel GSK-3β inhibitors. Read More

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http://dx.doi.org/10.2174/1871524918666180530074116DOI Listing
November 2018
34 Reads

Recent Findings in Melatonin Research and Their Relevance to the CNS.

Cent Nerv Syst Agents Med Chem 2018 ;18(2):102-114

Johann Friedrich Blumenbach Institute of Zoology and Anthropology, University of Goettingen, Goettingen, Germany.

Introduction: Several recent developments in melatonin research deserve attention and divulgation. The role of melatonin in the brain has been extended to its synthesis in the cerebellum as a response to inflammation, findings that exceed the earlier demonstration of aralkylamine Nacetyltransferase expression. The release of melatonin via the pineal recess into the third ventricle appears to be more important than previously believed and has been discussed as a strong direct signal to the suprachiasmatic nucleus. Read More

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http://dx.doi.org/10.2174/1871524918666180531083944DOI Listing
November 2018
2 Reads

Synthesis and Evaluation of 2-benzylidene-1-tetralone Derivatives for Monoamine Oxidase Inhibitory Activity.

Cent Nerv Syst Agents Med Chem 2018 ;18(2):136-149

Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.

Background: Chalcone has been identified as a promising lead for the design of Monoamine Oxidase (MAO) inhibitors. This study attempted to discover potent and selective chalcone-derived MAO inhibitors by synthesising a series consisting of various cyclic chalcone derivatives. The cyclic chalcones were selected based on the possibility that their restricted structures would confer a higher degree of MAO isoform selectivity, and included the following chemical classes: 1-indanone, 1- tetralone, 1-benzosuberone, chromone, thiochromone, 4-chromanone and 4-thiochromanone. Read More

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http://dx.doi.org/10.2174/1871524918666180501121638DOI Listing
November 2018
6 Reads

Nitrocatechol Derivatives of Chalcone as Inhibitors of Monoamine Oxidase and Catechol-O-Methyltransferase.

Cent Nerv Syst Agents Med Chem 2018 ;18(2):115-127

Pharmaceutical Chemistry, School of Pharmacy and Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.

Introduction: The efficacy of L-dopa in the treatment of Parkinson's disease depends on its metabolic conversion to dopamine in the brain, however extensive peripheral metabolism of L-dopa diminishes its availability for uptake into the brain. L-Dopa is extensively decarboxylated in the gastrointestinal tract and peripheral tissues by Aromatic L-Amino Acid Decarboxylase (AADC), and AADC inhibitors are thus frequently combined with L-dopa therapy. When AADC is inhibited, 3-Omethylation Catalysed by Catechol-O-Methyltransferase (COMT) becomes a dominant metabolic pathway for L-dopa, and COMT inhibitors may thus also be used as adjuncts to L-dopa in Parkinson's disease. Read More

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http://dx.doi.org/10.2174/1871524918666180426125714DOI Listing
November 2018
4 Reads

Evaluation of In Silico Anti-parkinson Potential of β-asarone.

Cent Nerv Syst Agents Med Chem 2018 ;18(2):128-135

Department of Pharmacology, Indo-Soviet Friendship College of Pharmacy (ISFCP), Moga, Punjab, India.

Introduction: Parkinson's disease is affecting millions of people worldwide. The prevalence of Parkinson's disease is 0.3% globally, rising to 1% in more than 60 years of age and 4% in more than 80 years of age and the figures are thought to be doubled by 2030. Read More

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http://dx.doi.org/10.2174/1871524918666180416153742DOI Listing
November 2018
25 Reads

Editorial: Current Strategies for Drug Discovery Targeting Neurological Autoimmune Diseases.

Cent Nerv Syst Agents Med Chem 2018 01;18(1)

Department of Immunology and Microbiology, School of Medicine, Wayne State University, Detroit, MI, United States.

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http://dx.doi.org/10.2174/187152491801180126155303DOI Listing
January 2018
6 Reads

Preface.

Cent Nerv Syst Agents Med Chem 2018 Jan;18(1)

Biopharma Research Leader Organic and Medical Chemist Registered US Patent Agent Catonsville, MD, United States.

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http://dx.doi.org/10.2174/187152491801180126155039DOI Listing
January 2018
7 Reads

ISATIN: New Hope Against Convulsion.

Cent Nerv Syst Agents Med Chem 2018 ;18(2):76-101

Department of Pharmaceutical Chemistry, H.R. Patel Institute of Pharmaceutical Education and Research, Shirpur, Dhule, 425405 Maharashtra, India.

Background: Epilepsy is one in every of the foremost important chronic neurological disorders with high incidence worldwide. Several epileptic patients don't seem to be fully treated with currently available marketed medicines likewise so many drugs have shown unfavorable side effect and drug interaction. Therefore, there are continuing interests to seek out new anticonvulsant drugs. Read More

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http://www.eurekaselect.com/157097/article
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http://dx.doi.org/10.2174/1871524917666171113124112DOI Listing
November 2018
34 Reads

Biomedical Application of Polymers: A Case Study of Non-CNS Drugs Becoming CNS Acting Drugs.

Cent Nerv Syst Agents Med Chem 2018 Jan;18(1):32-38

Department of Veterinary Physiology, Pharmacology and Biochemistry, College of Veterinary Medicine, University of Agriculture, P.M.B. 2373, Makurdi, Benue State, Nigeria.

Background: The transport of CNS acting drugs across blood-brain barrier (BBB) is complex and guided by the molecular weight, pH, physicochemical and pathological state of the BBB among others.

Methods: In view of this, literatures were assessed for possible conversion of Non-CNS to CNS acting drugs, whose ability to penetrate CNS can be improved using polymers for biomedical applications.

Results: The findings have shown that compounds with pyridine, pyrrole, carboxamide, pyridone among others can be converted to CNS acting drugs that can be loaded in specialized carrier polymers for transportation across BBB. Read More

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http://dx.doi.org/10.2174/1871524917666170821115748DOI Listing
January 2018
14 Reads

Editorial: Neurodegenerative Disorders: Synthesis, Drug Delivery Strategies and Biological Evaluation of New Therapeutic Agents.

Cent Nerv Syst Agents Med Chem 2017 ;17(2):89

Department of Medical and Oral Sciences and Biotechnologies, School of Medicine and Health Sciences, University "G.d'Annunzio" Chieti-Pescara, Chieti, Italy.

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http://dx.doi.org/10.2174/187152491702170712214058DOI Listing
August 2018
8 Reads