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


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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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 May 29. Epub 2018 May 29.

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 central nervous system (CNS). Dysregulation of Glycogen synthase kinase 3 (GSK-3) activity gives a 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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Recent Findings in Melatonin Research and Their Relevance to the CNS.

Cent Nerv Syst Agents Med Chem 2018 May 30. Epub 2018 May 30.

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

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 N-acetyltransferase 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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Synthesis and evaluation of 2-benzylidene-1-tetralone derivatives for monoamine oxidase inhibitory activity.

Cent Nerv Syst Agents Med Chem 2018 May 1. Epub 2018 May 1.

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

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

Cent Nerv Syst Agents Med Chem 2018 Apr 26. Epub 2018 Apr 26.

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

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-O-methylation 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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Evaluation of In Silico Anti-parkinson potential of β-asarone.

Cent Nerv Syst Agents Med Chem 2018 Apr 16. Epub 2018 Apr 16.

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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April 2018
2 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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January 2018
1 Read

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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January 2018
2 Reads

ISATIN: New hope against convulsion.

Cent Nerv Syst Agents Med Chem 2017 Nov 13. Epub 2017 Nov 13.

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

Epilepsy is one of the most significant chronic neurological disorders with high occurrence worldwide. Many epileptic patients are not completely treated with currently available marketed drugs as well as so many drugs have shown unfavorable side effect and drug interaction. Therefore, there are continuing interests to find new anticonvulsant drugs. Read More

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November 2017
8 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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January 2018
3 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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January 2017
2 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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June 2018
5 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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June 2018
2 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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June 2018
6 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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June 2018
6 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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June 2018
2 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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June 2018
5 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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June 2018
6 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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January 2018
2 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
2 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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June 2018
2 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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June 2018
6 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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January 2017
3 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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January 2018
2 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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January 2017
26 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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January 2017
6 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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January 2017
2 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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January 2017
4 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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January 2017
3 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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January 2017
35 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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January 2017
2 Reads

Synthesis and Antioxidant Properties of Novel Memantine Derivatives.

Cent Nerv Syst Agents Med Chem 2017 ;17(2):123-128

Department of Pharmacy, University "G. d'Annunzio" of Chieti-Pescara, Via dei Vestini 31, Chieti Scalo (CH), Italy.

Background: Medicinal chemistry methodologies are presently used to develop multifunctional molecules which simultaneously reduce oxidative stress, excitotoxicity, metal dyshomeostasis, and neuroinflammation that characterize neuropathological conditions, such as Alzheimer's Disease.

Results: Memantine (MEM) derivatives 1-6 were designed and synthesized as novel multifunctional entities with antioxidant and neuroprotective capabilities to manage neurodegenerative diseases, such as Alzheimer's Disease. In vitro neuroprotective studies were performed by using astroglial GL15 cell line to assess antioxidant capability of MEM derivatives 1-6. Read More

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January 2017
3 Reads

Editorial (Thematic Issue: Rational Approaches for the Design of Monoamine Oxidase Inhibitors).

Authors:
Bijo Mathew

Cent Nerv Syst Agents Med Chem 2016 ;16(2):74

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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February 2017
2 Reads

Understanding the Metabolic Consequences of Human Arylsulfatase A Deficiency through a Computational Systems Biology Study.

Cent Nerv Syst Agents Med Chem 2016 May 10. Epub 2016 May 10.

Institute for the Study of Inborn Errors of Metabolism, Facultad de Ciencias, Pontificia Universidad Javeriana, Cra 7 No. 43-82 Building 53, Room 303A. Bogotá, Colombia.

The nervous system is responsible for the communication between the organism and its environment. This task is possible by the presence of the myelin sheath, which is a double membrane formed by about 75% lipids and 25% proteins. The sulfatide represents one of the main lipids of the myelin band; its degradation is catabolized by the enzyme Arylsulfatase A (ARSA), to generated galactosylceramide. Read More

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May 2016
3 Reads

Astrocyte´s RAGE: More Than Just a Question of Mood.

Cent Nerv Syst Agents Med Chem 2018 Jan;18(1):39-48

Biomedical Sciences Research Group, School of Medicine, Universidad Antonio Narino, Bogota, Colombia.

Background: Adequate function of the nervous system depends on the balance of glianeuron complex interactions. Astrocytes, in particular, are key elements in this process due to the significant participation of these cells in essential properties of the nervous system such as neuroinflammation, regulation of neurotransmitters, release of gliotransmitters and control of synaptic plasticity, among others. Astrocytes express the receptor for advanced glycation end products (RAGE) which is very important in the recognition of endogenous molecules released in the context of infection, physiological stress or chronic inflammation. Read More

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January 2018
4 Reads

Toxicity of Mediterranean Scyphomedusae: An Overview.

Cent Nerv Syst Agents Med Chem 2016 ;16(3):213-217

OGS (Istituto Nazionale di Oceanografia e di Geofisica Sperimentale) - Trieste, Italy.

Following in-depth analysis and examination, jellyfish toxins have been found to consist of a mixture of proteins, carbohydrates, and other non-proteinaceous components. What remains to be clarified is the specific chemical nature of jellyfish toxins due to their heat lability. This paper reviews current knowledge of the toxic properties of the most common Mediterranean scyphozoans (A. Read More

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February 2017
5 Reads

Stimulated CB1 Cannabinoid Receptor Inducing Ischemic Tolerance and Protecting Neuron from Cerebral Ischemia.

Cent Nerv Syst Agents Med Chem 2017 ;17(2):141-150

Department of Pharmacology, School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China.

Background: It is reported that endogenous cannabinoids can cause vasodilation and bradycardia. They have anti-inflammatory effect and protect endothelial cells from injury, therefore they have potential application prospect in the prevention of cardio-cerebrovascular diseases. However, the mechanisms of the neuroprotection mediated by cannabinoid 1 receptors (CB1Rs) have not been uncovered in detail. Read More

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January 2017
13 Reads

Schiff Bases of Benzothiazol-2-ylamine and Thiazolo[5,4-b] pyridin-2-ylamine as Anticonvulsants: Synthesis, Characterization and Toxicity Profiling.

Cent Nerv Syst Agents Med Chem 2016 ;16(3):240-248

Faculty of Pharmacy, Babu Banarasi Das Northern India Institute of Technology, Sector-2, Dr. Akhilesh Das Nagar, Faizabad Road, Lucknow, 227105, U.P., India.

Background: Schiff bases have a broad spectrum of biological activities like antiinflammatory, analgesic, antimicrobial, anticonvulsant, antitubercular, anticancer, antioxidant, anthelmintic and so forth. Thus, after a thorough perusal of literature, it was decided to conjugate benzothiazol-2-ylamine/thiazolo [5, 4-b] pyridin-2-ylamine with aromatic and heteroaromatic aldehydes to get a series of Schiff bases.

Objective: Synthesis, characterization, in-silico toxicity profiling and anticonvulsant activity of the Schiff bases of Benzothiazol-2-ylamine and Thiazolo [5, 4-b] pyridin-2-ylamine. Read More

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February 2017
5 Reads

Physiological targets for the treatment of diabetic encephalopathy.

Cent Nerv Syst Agents Med Chem 2016 Apr 28. Epub 2016 Apr 28.

Ceara State University Av. Dr. Silas Munguba, 1700, Campus do Itaperi, Fortaleza-CE.

Background: Diabetes mellitus is a chronic degenerative disease responsible for hyperglycemic episodes through insulin secretion deficiency or cellular resistance. Clinical diagnosis in diabetic patients established that this disease affects the CNS, damaging the brain and impairing cognition, and thus establishing a clinical diabetic condition named diabetic encephalopathy. Despite the physiological mechanisms responsible for the development diabetic encephalopathy are still unclear, an excessive formation of reactive oxygen species, an alteration of acetylcholinesterase activity, and a reduction of growth factor levels, may be related with the pathogenesis of this condition. Read More

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April 2016
7 Reads

Drug Design Strategies for the Discovery of Novel Anticonvulsants Concerned with Four Site Binding Pharmacophoric Model Studies.

Cent Nerv Syst Agents Med Chem 2016 Apr 11. Epub 2016 Apr 11.

Institute of Pharmaceutical Sciences, Guru Ghasidas University, Bilaspur, India.

Anticonvulsant refers to a group of pharmaceuticals used in the treatment of epileptic seizures. The use of current antiepileptic drugs has been questioned due to the non-selectivity of the drugs and the undesirable side effects produced by them. This led to the search for antiepileptic compounds with more selectivity and lower toxicity. Read More

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April 2016
3 Reads

Novel pyrimidine based semicarbazones: Confirmation of four binding site pharmacophoric model hypothesis for antiepileptic activity.

Cent Nerv Syst Agents Med Chem 2016 Mar 30. Epub 2016 Mar 30.

Institute of Pharmaceutical Sciences, Guru Ghasidas University, Bilaspur, India.

Background: Epilepsy is a neurological disorder, characterized by seizures accompanied by loss or disturbance of consciousness affecting various physical and mental functions. Current anticonvulsant drugs are effective in controlling seizures in about 70% of cases, but their use is often limited by side effects like ataxia, megaloblastic anemia, hepatic failure. In search for a novel anticovulsant drug with better efficacy and lower toxicity, a series of novel pyrimidine based semicarbazone were designed and evaluated for antiepileptic activity. Read More

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March 2016
6 Reads

Analgesic Effects Mediated by Muscarinic Receptors: Mechanisms and Pharmacological Approaches.

Cent Nerv Syst Agents Med Chem 2016 ;16(3):218-226

Department of Biology and Biotechnologies Charles Darwin, Research Center of Neurobiology Daniel Bovet, Sapienza, University of Rome, P.le A. Moro, 5-00185 Roma, Italy.

Chronic pain represents a research field on great clinical relevance and social impactful. It is associated to a variety of pathological events causing un altered excitability of peripheral nerves derived by tissue damage depending on physical, biological and chemical injury. In the last years much attention has been paid in the identification of novel molecules involved in mediating pain sensation useful as therapeutic tools for the development of new analgesic drugs. Read More

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February 2017
2 Reads

Diagnostic Value of CRP, Procalcitonin, and Ferritin Levels in Cerebrospinal Fluid of Children with Meningitis.

Cent Nerv Syst Agents Med Chem 2018 Jan;18(1):58-62

Dental Research Center, Dentistry Research Institute, Department of Community Oral Health, School of Dentistry, Tehran University of Medical Sciences, Tehran, Iran.

Background And Objective: Bacterial meningitis is a serious disease with high rate of mortality and morbidity in children. Invasion of pathogens causes brain and meningeal inflammation, which leads to the release of biomarkers into cerebrospinal fluid (CSF). Identification of these biomarkers can help the physicians to differentiate between bacterial and aseptic meningitis. Read More

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January 2018
3 Reads

Topiramate: A Novel Therapeutic Candidate for Diabetes and Aggression? Positron Emission Tomography (PET) Findings.

Cent Nerv Syst Agents Med Chem 2016 ;16(3):227-230

Department of Neurology University of Istanbul-Medipol, Istanbul, Turkey.

Background: There is still limited knowledge regarding the role of impaired brain glucose metabolism in the generation of aggression during diabetes. Additionally, there are rapidly replicating piece of evidence suggesting that topiramate may exert significant mood stabilizing effect. In this respect, we aimed to evaluate the neurometabolic correlates of the therapeutic effect of topiramate in a patient with diabetes and Intermittent explosive disorder (IED). Read More

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February 2017
8 Reads

Neuromyelitis Optica (NMO IgG+) and Genetic Susceptibility, Potential Ethnic Influences.

Cent Nerv Syst Agents Med Chem 2018 Jan;18(1):4-7

Neurodegenerative Diseases Department, Instituto Nacional de Neurologia y Neurocirugia Manuel Velasco Suarez, Mexico City, Mexico.

Introduction: Neuromyelitis optica (NMO) and Multiple Sclerosis (MS) have been reported in different populations. NMO is more frequent in non-Caucasians, and clinical phenotype differences between populations are likely influenced by genetic susceptibility. In Brazil, it has been reported that NMO patients have a mainly European ancestry background. Read More

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January 2018
35 Reads

Epigenetics in Multiple Sclerosis: Molecular Mechanisms and Dietary Intervention.

Cent Nerv Syst Agents Med Chem 2018 Jan;18(1):8-15

Laboratory of Clinical Neurodegenerative Diseases, National Institute of Neurology and Neurosurgery of Mexico, Insurgentes Sur # 3877, CP 14269 Mexico City, Mexico.

Introduction: Multiple Sclerosis (MS) is a chronic, inflammatory, neurodegenerative demyelinating disease of the central nervous system (CNS). Unfortunately, MS causes important disability in young adults and its prevalence is increasing. While the etiology of MS etiology is not completely understood, it seems to be a multifactorial entity that is influenced by both genetic and epigenetic modifications. Read More

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January 2018
2 Reads

Thiophene Scaffold as Prospective Central Nervous System Agent: A Review.

Cent Nerv Syst Agents Med Chem 2016 ;16(2):158-64

Department of Pharmaceutical Sciences, Chaudhary Bansi Lal University, Bhiwani-127021, India.

Background: Heterocyclic compounds are extensively dispersed in nature and are vital for life. Various investigational approaches towards Structural Activity Relationship that focus upon the exploration of optimized candidates have become vastly important.

Method: Literature studies tell that for a series of compounds that are imperative in industrial and medicinal chemistry, thiophene acts as parent. Read More

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February 2017
3 Reads

Analgesic and CNS Depressant Activities of Sea Anemone Heteractis aurora Nematocyst Toxin.

Cent Nerv Syst Agents Med Chem 2016 ;16(3):167-172

Marine Biotoxinology Lab. Centre of Advanced Study in Marine Biology, Faculty of Marine Sciences, Annamalai University, Parangipettai - 608 502, Tamil Nadu, India.

Marine organisms are the excellent sources for biologically active compounds. Cnidarian venoms are potentially valuable materials used for biomedical research and drug development. The present work was carried out to analyse haemolytic, analgesic and CNS depressant activity of sea anemone Heteractis aurora. Read More

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February 2017
3 Reads

Thiazolidine: A Potent Candidate for Central Nervous Systems Diseases.

Cent Nerv Syst Agents Med Chem 2016 Jan 6. Epub 2016 Jan 6.

Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi -835215, Jharkhand, India.

Thiazolidines are multifaceted molecules and exhibit varied types of biological activities, and also showed anticonvulsants and antidepressants activity. It is the diversified class of heterocyclic compounds. Thiazolidinediones (TZD) has been shown beneficial action in various CNS diseases. Read More

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January 2016
2 Reads