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


Preface.

Authors:
Gjumrakch Aliev

Cent Nerv Syst Agents Med Chem 2019 ;19(1):3-5

Department of Pharmacology and Pharmacy Sechenov University, 119991, Moscow, Russian Federation.

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http://dx.doi.org/10.2174/187152491901190318092003DOI Listing
January 2019
1 Read

Aging Affects Nicotinic Acetylcholine Receptors in Brain.

Authors:
Yuri N Utkin

Cent Nerv Syst Agents Med Chem 2019 Mar 19. Epub 2019 Mar 19.

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
March 2019
1 Read

Pharmacological approach of Pistacia vera fruit as learning and memory potential in chemically induced memory impairment mice.

Cent Nerv Syst Agents Med Chem 2019 Mar 4. Epub 2019 Mar 4.

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
March 2019
1 Read

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

Cent Nerv Syst Agents Med Chem 2019 Feb 27. Epub 2019 Feb 27.

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

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. 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
February 2019
2 Reads

Natural Compounds and Drug Discovery. Can Cnidarian Venoms Play a Role?

Cent Nerv Syst Agents Med Chem 2019 Feb 27. Epub 2019 Feb 27.

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
February 2019

Acrylamide induced toxicity and the propensity of Phytochemicals in amelioration: a review.

Cent Nerv Syst Agents Med Chem 2019 Feb 7. Epub 2019 Feb 7.

School of Basic and Applied Sciences, Department of Biological 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
February 2019
5 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
January 2019

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
January 2019
9 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
January 2019
20 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
January 2019
10 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
January 2019
16 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
January 2019
16 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
January 2019
2 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 Aug 29. Epub 2018 Aug 29.

Department of Medical Physics and Biomedical Engineering, School of Medicine (International Campus), Tehran University of Medical Science, Tehran. Iran.

Peripheral nerve lesion is a common clinical problem that may produce long-term functional defects. Usually, crush injuries, fractures, scars, lacerations, compression, or iatrogenic reasons are reasons of 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
August 2018
20 Reads

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

Cent Nerv Syst Agents Med Chem 2018 08 26. Epub 2018 Aug 26.

Sechenov First Moscow State Medical University, 119991, Moscow. Russian Federation.

One promising target for novel psychotropic drugs is the 5-HT6 receptor, G-protein-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 pro-cognitive effects. 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
August 2018
17 Reads

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

Authors:
Yuri Utkin

Cent Nerv Syst Agents Med Chem 2018 Aug 13. Epub 2018 Aug 13.

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
August 2018
7 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 Jul 16. Epub 2018 Jul 16.

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
July 2018
3 Reads

Neuropharmacological profile of gamma-decanolactone on chemically-induced seizure in mice.

Cent Nerv Syst Agents Med Chem 2018 Jun 10. Epub 2018 Jun 10.

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
June 2018
5 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
12 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
5 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
3 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
21 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
4 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
5 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
29 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
10 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
4 Reads

Novel Mannich-bases as Potential Anticonvulsants: Syntheses, Characterization and Biological Evaluation.

Cent Nerv Syst Agents Med Chem 2017 ;17(3):219-228

Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, Sector-2, Dr. Akhilesh Das Nagar, Faizabad Road, Lucknow, 226028, U.P.. India.

Background: Mannich bases are known to be an important pharmacophore or bioactive leads in the synthesis of various potential agents that have a variety of therapeutic activities like anticancer, antipsychotic, anticonvulsant, antimalarial, anti-inflammatory, antibacterial and so forth. Thus, in the present research, conjugation of moieties like 1,5-benzoxazepines and 1,5-benzothiazepines with secondary amines like piperazine, methyl piperazine and morpholine was carried out in a Mannich base with an anticipation of good anticonvulsant activity.

Objective: Synthesis, characterization, structure activity relationship and anticonvulsant activity of the Mannich bases of 1,5-benzothiazepine and 1,5-benzoxazepine derivatives. Read More

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http://www.eurekaselect.com/154240/article
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http://dx.doi.org/10.2174/1871524917666170717113524DOI Listing
June 2018
62 Reads

Synthesis and Evaluation of Novel Diazaspiro Hydantoins as Potential Anticonvulsants.

Cent Nerv Syst Agents Med Chem 2017 ;17(3):201-208

Department of Basic Science, School of Engineering and Technology, Jain University Bangalore. India.

Background: Epilepsy, one of the most frequent neurological afflictions in man characterized by excessive temporary neuronal discharges resulting in uncontrolled convulsion, requires special medical attention. Though several new anticonvulsants are introduced, some types of seizures are still not adequately treated with current therapy. Toxicity, intolerance, and lack of efficacy for certain types of seizure are some of the limitations of the current medications. Read More

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http://dx.doi.org/10.2174/1871524917666170712111508DOI Listing
June 2018
9 Reads

Functional Chemical Groups that May Likely Become a Source for the Synthesis of Novel Central Nervous System (CNS) Acting Drugs.

Cent Nerv Syst Agents Med Chem 2017 ;17(3):178-186

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

Introduction: Central Nervous System (CNS) disorders are on increase perhaps due to genetic, enviromental, social and dietetic factors. Unfortunately, a large number of CNS drugs have adverse effects such as addiction, tolerance, psychological and physical dependence. In view of this, literature search was carried out with a view to identify functional chemical groups that may serve as lead molecules for synthesis of compounds that may have CNS activity. Read More

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http://dx.doi.org/10.2174/1871524917666170502153752DOI Listing
June 2018
20 Reads

Homology Modeling Inspired Synthesis of 5-HT2A Receptor Inhibitors: A Diazepine Analogue of the Atypical Antipsychotic JL13.

Cent Nerv Syst Agents Med Chem 2017 ;17(3):239-244

Clinical and Translational Science Institute, Tufts University Medical Center, 800 Washington Street, Boston, MA 02111. United States.

Background: The benzoxazepine JL13 is an analogue of the clozapine family of antipsychotic agents which target the 5-HT2A receptor, and has showed promise as an atypical antipsychotic agent. Based on the dearth of clinically effective anti-psychotic agents available, we sought to design and chemically synthesize additional analogues.

Methods: Structure function analysis was conducted using state of art computational methods, which were designed to highlight new candidates for chemical synthesis. Read More

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http://dx.doi.org/10.2174/1871524917666170426123607DOI Listing
June 2018
15 Reads

Investigation on the Molecular Interactions Stabilizing the Structure of α-synuclein Fibril: An In silico Study.

Cent Nerv Syst Agents Med Chem 2017 ;17(3):209-218

Molecular Modelling and Simulation Laboratory, Department of Molecular Biology and Biotechnology, Tezpur University, Tezpur-784 028, Assam. India.

Background: Amyloid fibrils represent stable form of many misfolded proteins associated with numerous diseases like Parkinson's Disease (PD), Type II diabetes and Alzheimer's disease (AD). α-synuclein protein is the principal constituent of Lewy bodies that are considered to be pathological hallmark of PD. Recently, a high resolution structure of α-synuclein protein that stacks together forming fibrils in brains of PD patients were identified. Read More

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http://dx.doi.org/10.2174/1871524917666170427152849DOI Listing
June 2018
8 Reads

Synthesis, Computational and Pharmacological Evaluation of N-(2-benzoyl- 4-chlorophenyl)-2-(4-(Substituted Phenyl) Piperazin-1-yl) Acetamides as CNS Agents.

Cent Nerv Syst Agents Med Chem 2017 ;17(3):229-238

Faculty of Pharmacy, IFTM University, Moradabad-244001(U.P.). India.

Background: A series of new N-(2-benzoyl-4-chlorophenyl)-2-(4-(substituted phenyl) piperazin-1-yl) acetamides (3a-j) have been synthesized by the chloroacetylation of 2-amino-5- chlorbenzophenone which was further reacted with substituted phenylpiperazine.

Material: The chemical structures of the compounds were confirmed on the basis of their TLC, IR, 1HNMR, 13CNMR and by elemental analysis. The physicochemical similarity of the target compounds with respect to standard drug diazepam was assessed by calculating from a set of physicochemical properties using software programs. Read More

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http://dx.doi.org/10.2174/1871524917666170321103951DOI Listing
June 2018
13 Reads

Green Tea (Camellia sinensis) Protects Against Arsenic Neurotoxicity via Antioxidative Mechanism and Activation of Superoxide Dismutase Activity.

Cent Nerv Syst Agents Med Chem 2017 ;17(3):187-195

Department of Nutrition, Raja N.L Khan Women's College, Midnapore, West Bengal. India.

Background: Chronic arsenic-exposure even at a low-dose results in the neural impairment and motor/cognitive dysfunction. However, several preventive approaches are made mainly against hepatic/ gastrointestinal damages. Only a few investigations postulate therapeutic strategies for neural anomalies. Read More

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http://dx.doi.org/10.2174/1871524917666170201145102DOI Listing
June 2018
11 Reads

Synthesis, Molecular Docking and Evaluation of 3-{4-[2-amino-4-(substitutedphenyl)-2H-[1, 3] oxazin/thiazin-6-yl} 2-phenyl-3H-quinazolin-4-one Derivatives for their Anticonvulsant Activity.

Cent Nerv Syst Agents Med Chem 2018 Jan;18(1):63-73

Computational & Synthetic Chemistry Division, Department of Pharmaceutical Chemistry, VNS Group of Institutions- Faculty of Pharmacy, Neelbud, Bhopal- 462023 (M.P.), India.

Background: According to the WHO, around 50 million people worldwide are suffering from epilepsy. It is due to the repeated occurring of seizures. These seizures are caused by sudden which may vary from a brief lapse of attention or muscle jerks, to severe and prolonged convulsions. Read More

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http://dx.doi.org/10.2174/1871524917666170104142033DOI Listing
January 2018
6 Reads

Editorial (Thematic Issue: The Activity of Products From Cnidaria: A Therapeutic Tool in Neurological Diseases? Part II).

Cent Nerv Syst Agents Med Chem 2016 ;16(3):165-166

Central Nervous System Agents in Medicinal Chemistry Department of Earth, Environment and Life Sciences (DISTAV) University of Genova Viale Benedetto XV 5, I-16132, Genova, Italy.

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February 2017
5 Reads

In vivo Piroxicam Metabolites: Possible Source for Synthesis of Central Nervous System (CNS) Acting Depressants.

Cent Nerv Syst Agents Med Chem 2017 ;17(3):172-177

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

Background: Piroxicam has been reported to be convertible to Central Nervous System (CNS) acting agents. It has serious depressant effects at high doses.

Objective: In view of this, structures of piroxicam metabolites were assessed for possible conversion to CNS depressants. Read More

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http://dx.doi.org/10.2174/1871524917666161111093759DOI Listing
June 2018
8 Reads

Pharmacological Evaluation of the Recuperative Effect of Morusin Against Aluminium Trichloride (AlCl3)-Induced Memory Impairment in Rats.

Cent Nerv Syst Agents Med Chem 2017 ;17(3):196-200

School of Biomedical Sciences and Pharmacy, University of Newcastle, Newcastle, NSW 2308. Australia.

Background: Elevation in brain levels of aluminium can be neurotoxic and can cause learning and memory deficiencies. In Chinese medicine, Morus alba is used as a neuroprotective herb. The current study was intended to discover the recuperative effect of morusin against aluminium trichloride (AlCl3)-induced memory impairment in rats along with biochemical mechanism of its protective action. Read More

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http://dx.doi.org/10.2174/1871524917666161111095335DOI Listing
June 2018
30 Reads

Design, Synthesis and Molecular Docking Studies of New Potential Piperazine Derivatives as Cognition Enhancers.

Cent Nerv Syst Agents Med Chem 2017 ;17(2):157-170

University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh-160 014, India.

Background: In 2016, the statistical reports stated that Alzheimer is not just memory loss but it kills and has become the 6th leading cause of death. The number of dementia patients is increasing rapidly and expected to rise to 131.5 million by 2050. Read More

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http://dx.doi.org/10.2174/1871524916666161014123016DOI Listing
September 2018
9 Reads

Basic Approaches in Therapy of Multiple Sclerosis (MS) and Related Diseases: Current Achievement and Prospective.

Cent Nerv Syst Agents Med Chem 2018 Jan;18(1):21-31

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

Introduction: This overview is aimed at reevaluating fundamental approaches of current MS therapies with focus being placed on their targeted underlying immune, molecular and cellular mechanisms. Currently used therapies are discussed in regard to their mechanisms of action, clinical accomplishments and unwanted side effects and complications. Special emphasis is given to the current first generation Disease Modifying Therapies (DMT) and their actions at immune mechanisms of disease. Read More

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http://dx.doi.org/10.2174/1871524916666161018102254DOI Listing
January 2018
6 Reads

Role of the α7 Nicotinic Acetylcholine Receptor and RIC-3 in the Cholinergic Anti-inflammatory Pathway.

Cent Nerv Syst Agents Med Chem 2017 ;17(2):90-99

Department of Neurology, The Agnes Ginges Center for human Neurogenetics, Hadassah University Hospital and Hebrew University Medical School, Jerusalem, Israel.

Background: The nicotinic acetylcholine receptor (nAChR) gene family encodes for subunits of acetylcholine gated ion channels. These receptors are expressed widely and have many functions: They mediate excitation at neuro-muscular junctions. Nicotinic Acetylcholine Receptor: In the central nervous system nAChRs have been implicated in memory, cognition, and addiction. Read More

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http://dx.doi.org/10.2174/1871524916666160829114533DOI Listing
September 2018
50 Reads

Anticancer, Antioxidant and Cytotoxic Potential of Thymol in vitro Brain Tumor Cell Model.

Cent Nerv Syst Agents Med Chem 2017 ;17(2):116-122

Department of Soil Science and Plant Nutrition, Faculty of Agriculture, Ataturk University, TR-25240, Erzurum, Turkey.

Background: Thymol (THY), which is a monocyclic monoterpene, found in oil of thyme various other kinds of plants. Until today, although different biological properties of THY have been indicated, its neurological toxicity has never been investigated.

Method: In this study, in vitro antiproliferative (by 3-(4,5 dimetylthiazol-2-yl)-2,5 diphenlytetrazolium bromide (MTT) test), genotoxic (by single cell gel electrophoresis (SCGE)) and oxidative effects (by total antioxidant capacity (TAC) and total oxidative status (TOS) analysis) of THY (0-400 mg/L) were assessed on cultured primary rat neurons (CPRNs) and N2a neuroblastoma cells. Read More

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http://dx.doi.org/10.2174/1871524916666160823121854DOI Listing
September 2018
27 Reads

Effect of MRJF4 on C6 Glioma Cells Proliferation and Migration.

Cent Nerv Syst Agents Med Chem 2017 ;17(2):129-134

Department of Drug Sciences, Medicinal Chemistry Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.

Background: MRJF4, a novel haloperidol metabolite II prodrug, was obtained through the esterification of the secondary hydroxyl group of haloperidol metabolite II with 4-phenylbutyric acid. The activities of (±)-MRJF4 and its two enantiomers [(+)-MRJF4 and (-)-MRJF4] as tumor specific inducers of pro-apoptotic genes were evaluated on malignant C6 glioma cells. In particular, changes in Nf-κB signaling pathway, activity of nitric oxide synthases (NOS), metalloproteinases (MMPs), and membrane adhesion proteins were investigated. Read More

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http://dx.doi.org/10.2174/1871524916666160823122712DOI Listing
September 2018
18 Reads

Cholinergic System and Neuroinflammation: Implication in Multiple Sclerosis.

Cent Nerv Syst Agents Med Chem 2017 ;17(2):109-115

Department of Biology and Biotechnologies C. Darwin, Research Center of Neurobiology Daniel Bovet, "Sapienza" University of Rome, Italy.

Background: Multiple sclerosis (MS) is an inflammatory and neurodegenerative disease of the central nervous system (CNS) characterized by leucocytes infiltration, demyelination, axonal degeneration and neuronal death. Although the etiology of MS is still unkwon, inflammation and autoimmunity are considered to be key players of the disease. Nervous System: The severe alterations affecting the nervous system contribute to the motor and cognitive disabilities and are in large part dependent on severe inflammatory processes active in both central nervous system and immune system. Read More

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http://dx.doi.org/10.2174/1871524916666160822115133DOI Listing
September 2018
7 Reads

How Valid is Placebo in the Indian Setting?

Cent Nerv Syst Agents Med Chem 2017 ;17(2):151-156

Department of Psychiatry, PS Medical College & SK Hospital, Karamsad, Anand, Gujarat, India.

Background: The Placebo is defined as an inert substance with a potent therapeutic effect. Its effect is attributed to its psychological and neurobiological effect. Its use in Psychiatric drug practice, drug trials and clinical practice is common, especially in India. Read More

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http://dx.doi.org/10.2174/1871524916666160810162420DOI Listing
September 2018
6 Reads

Alpha-7 Nicotinic Receptors in Nervous System Disorders: From Function to Therapeutic Perspectives.

Cent Nerv Syst Agents Med Chem 2017 ;17(2):100-108

Dipartimento di Biologia e Biotecnologie Charles Darwin, Centro di ricerca in Neurobiologia Daniel Bovet "Sapienza", Università di Roma, P.le A. Moro, 5-00185 Roma, Italy.

Background: The α7 nicotinic receptor consists of identical subunits and is one of the most abundant acetylcholine receptors in the mammalian central nervous system. However its expression is also found in the peripheral nervous system as well as in the immune system and various peripheral tissues. Nicotinic Receptors: They are involved in the regulation of several activities ranging from excitatory neurotransmission, the modulation of the release of several neurotransmitters, regulation of neurite outgrowth, and even neuronal survival/death. Read More

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http://dx.doi.org/10.2174/1871524916666160729111446DOI Listing
September 2018
40 Reads

Piroxicam: Source for Synthesis of Central Nervous System (CNS) Acting Drugs.

Cent Nerv Syst Agents Med Chem 2017 ;17(2):135-140

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

Background: The use of central nervous system (CNS) acting drugs in the management of neuro degenerative and psychiatric problems cannot be overemphasized. Therefore, the chemical structure of piroxicam can be modified to yield new CNS stimulants and depressants that can be of great benefit to man and animals.

Methodology: Acetylcholine has Methyl - Oxygen-Oxygen (M-O-O) and Nitrogen (N) functional groups which are structurally related to Sulphur-Oxygen-Oxygen (S-O-O) and Nitrogen (N) of piroxicam that are either methylated or hydrogenated. Read More

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http://dx.doi.org/10.2174/1871524916666160719102335DOI Listing
September 2018
6 Reads