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Central Nervous System Agents in Medicinal Chemistry

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https://www.readbyqxmd.com/read/29141569/isatin-new-hope-against-convulsion
#1
Rameshwar S Cheke, Sandip D Firke, Ravindra R Patil, Sanjay B Bari
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. Recently, there has been wide interest in compounds containing the isatin moiety with diverse biological effects. In view of the previous continuation of an ongoing program aiming at finding new structure leads to potential anticonvulsant activities, we are trying to compile recent efforts which have been made in the design and development of isatin derived anticonvulsant agents...
November 13, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28828968/biomedical-application-of-polymers-a-case-study-of-non-cns-drugs-becoming-cns-acting-drugs
#2
Saganuwan Alhaji Saganuwan
The transport of CNS acting drugs across blood-brain barrier is complex and guided by the molecular weight, PH, physicochemical and pathological state of the BBB among others. 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. 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...
August 20, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28714383/novel-mannich-bases-as-potential-anticonvulsants-syntheses-characterization-and-biological-evaluation
#3
Amit Kumar Keshari, Aseem Tewari, Shweta Singh Verma, Shailendra K Saraf
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...
July 17, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28707581/synthesis-and-evaluation-of-novel-diazaspiro-hydantoins-as-potential-anticonvulsants
#4
C S Ananda Kumar, B Veeresh, K C Ramesha, C S Ashok Raj, K M Mahadevaiah, S B Benaka Prasad
A series of novel diazaspiro compounds 6a-t were synthesised and biologically evaluated for their anticonvulsant activity in the maximal electroshock seizure (MES) assay. Most of the tested compounds exhibited moderate to weak activity in the MES screen test, The compounds 6f, 6h, 6i, 6j, 6p, 6s and 6n able to protect seizure effect significantly higher and this effect was similar when compared to standard drug treated rats.
July 12, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28464765/functional-chemical-groups-that-may-likely-become-source-for-synthesis-of-novel-central-nervous-system-cns-acting-drugs
#5
Saganuwan Alhaji Saganuwan
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 identifying functional chemical groups that may serve as lead molecule for synthesis of compounds that may have CNS activity. The search revealed that heterocycles that have heteroatoms such as nitrogen (N), sulphur (S) and oxygen (O) form the largest class of organic compounds...
May 2, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28460628/investigation-on-the-molecular-interactions-stabilizing-the-structure-of-%C3%AE-synuclein-fibril-an-in-silico-study
#6
Airy Sanjeev, Venkata Satish Kumar Mattaparthi
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). Lewy Bodies(LB) are the pathological hallmark of PD where long fibrils disrupting the brain's activity that constitutes the main component, α-synuclein. However α-synuclein structure has eluded researchers due to its complexity, insolubility and difficulty of characterizing one protein within a fibril. Recently, a high resolution structure of α-synuclein protein that stacks together forming fibrils in brains of PD patients was identified...
April 27, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28462720/homology-modeling-inspired-synthesis-of-5-ht2a-receptor-inhibitors-a-diazepine-analogue-of-the-atypical-antipsychotic-jl13
#7
Enrico Mongeau, Gengyang Yuan, Zachary Minden, Scott Waldron, Raymond Booth, Daniel Felsing, Mary Jo Ondrechen, Graham B Jones
The benzoxazepine JL13 is an analogue of the clozapine family which targets the 5-HT2A receptor, and has showed promise as an atypical antipsychotic agent. Following structure function analysis with a series of synthetic analogues, homology modeling was performed to determine key interaction sites with the receptor. An aza analogue was synthesized for evaluation, and demonstrated seventeen times greater affinity for the receptor. An improved synthetic route was developed to allow rapid modifications of the core and synthesis of related libraries...
April 26, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28325152/synthesis-computational-and-pharmacological-evaluation-of-n-2-benzoyl-4-chlorophenyl-2-4-substituted-phenyl-piperazin-1-yl-acetamides-as-cns-agents
#8
Shweta Verma, Surendra Kumar, Sushil Kumar
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. 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...
March 21, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28155600/green-tea-camellia-sinensis-protects-against-arsenic-neurotoxicity-via-antioxidative-mechanism-and-activation-of-superoxide-dismutase-activity
#9
Smarajit Maiti, Nirmallya Acharyya, Tamal K Ghosh, Sk Sajed Ali, Emili Manna, Aarifa Nazmeen, Nirmalya K Sinha
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. Here, the protective role of Green tea (Camellia sinensis or CS; 10mg/ml aqueous) has been evaluated against arsenic-induced (0.6ppm/100g bw/28 days) cerebral/cerebellar tissue degeneration, oxidative-threats and neurotransmitter deregulation in female rats...
February 1, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056730/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
#10
Nimisha Jain, Jugnu Jaiswal, Ashish Pathak, Pradeep Kumar Singour
BACKGROUND: According to World Health Organization (WHO), around 50 million people worldwide suffering from epilepsy. Therefore, continued search for safer and more effective anticonvulsants is urgently necessary. OBJECTIVES: The present work was to synthesize 2-phenyl substituted quiazolinone derivatives and to evaluate them for anticonvulsant activity and neurotoxic. METHODS: A series of novel 3-{4-[2-amino-4-(substitutedphenyl)-2H-[1.3] oxazin/thiazin-6-yl} 2-phenyl-3H-quinazolin-4-one derivatives were synthesized and evaluated for their anticonvulsant activity...
January 4, 2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28820058/editorial-neurodegenerative-disorders-synthesis-drug-delivery-strategies-and-biological-evaluation-of-new-therapeutic-agents
#11
EDITORIAL
Antonio Di Stefano, Marcella Reale
No abstract text is available yet for this article.
2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27573666/role-of-the-%C3%AE-7-nicotinic-acetylcholine-receptor-and-ric-3-in-the-cholinergic-anti-inflammatory-pathway
#12
Treinin Millet, Papke L Roger, Nizri Eran, Ben-David Yael, Mizrachi Tehila, Brenner Talma
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. And in non-excitatory cells they regulate differentiation, proliferation and inflammatory responses. The CHRNA7 gene encodes for the α7 nAChR subunit that assembles into a homomeric receptor having unusual properties...
2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27554922/anticancer-antioxidant-and-cytotoxic-potential-of-thymol-in-vitro-brain-tumor-cell-model
#13
Elanur Aydın, Hasan Turkez, Sener Tasdemir, Fazıl Hacımuftuoglu
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...
2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27554921/effect-of-mrjf4-on-c6-glioma-cells-proliferation-and-migration
#14
Stephanie Pacella, Jole Fiorito, Ivana Cacciatore, Viviana di Giacomo, Antonia Patruno, Monica Rapino, Antonio Di Stefano, Lisa Marinelli, Erika Fornasari, Amelia Cataldi, Orazio Prezzavento, Agostino Marrazzo
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...
2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27550615/cholinergic-system-and-neuroinflammation-implication-in-multiple-sclerosis
#15
Maria Di Bari, Giovanni Di Pinto, Marcella Reale, Guadalupe Mengod, Ada Maria Tata
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...
2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27514542/how-valid-is-placebo-in-the-indian-setting
#16
Himanshu Sharma, Bharti Sharma
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. Currently there is a debate whether to use it or not as there are ethical, moral and legal issues. Also, its mechanism of action is not known. DISCUSSION: The Indian Psychiatry scenario is muddled in relation to use of placebo in Randomized Controlled Trials or Psychiatric clinical practice...
2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27488345/alpha-7-nicotinic-receptors-in-nervous-system-disorders-from-function-to-therapeutic-perspectives
#17
Antonella De Jaco, Laura Bernardini, Jessica Rosati, Ada Maria Tata
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...
2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27439371/piroxicam-source-for-synthesis-of-central-nervous-system-cns-acting-drugs
#18
Saganuwan Alhaji Saganuwan
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...
2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27356627/synthesis-and-antioxidant-properties-of-novel-memantine-derivatives
#19
Erika Fornasari, Lisa Marinelli, Antonio Di Stefano, Piera Eusepi, Hasan Turkez, Stefania Fulle, Ester S Di Filippo, Andrea Scarabeo, Silvia Di Nicola, Ivana Cacciatore
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...
2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27142423/stimulated-cb1-cannabinoid-receptor-inducing-ischemic-tolerance-and-protecting-neuron-from-cerebral-ischemia
#20
Quankun Zhuang, Cailing Dai, Linglong Yang, Huimin Wen, Hongyun Wang, Xiaoxue Jiang, Yuyang Zhang
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. METHODS: Nearly one hundred of new publications relevant to the theme are almost selected from Pubmed...
2017: Central Nervous System Agents in Medicinal Chemistry
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