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Central Nervous System Agents in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28714383/novel-mannich-bases-as-potential-anticonvulsants-syntheses-characterization-and-biological-evaluation
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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/27834137/in-vivo-piroxicam-metabolites-possible-source-for-synthesis-of-central-nervous-system-cns-acting-depressants
#9
Saganuwan Alhaji Saganuwan
Piroxicam has been reported to be convertible to central nervous system (CNS) acting agents. It has serious depressant effects at high doses. In view of this structures of piroxicam metabolites were assessed for possible conversion to CNS depressants. Structural barbituric compounds, carboxamide, cyclohydrated, benzothiazone and carboxybenzothiazone metabolites which may act via dopamine and adrenergic receptors causing depression of CNS activities.
November 10, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27834136/pharmacological-evaluation-of-the-recuperative-effect-of-morusin-against-aluminium-trichloride-alcl3-induced-memory-impairment-in-rats
#10
Gaurav Gupta, Dinesh K Chellappan, Mohit Agarwal, Madhu Ashwathanarayana, Srinivas Nammi, Kavita Pabreja, Kamal Dua
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. METHODS: Memory deficiency was produced by AlCl3 (100 mg/kg; p.o.) in experimental animals...
November 10, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27758698/basic-approaches-in-therapy-of-multiple-sclerosis-ms-and-related-diseases-current-acchievements-and-prospective
#11
Dusanka Skundric
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 current disease modifying therapies (DMT) and their actions at immune mechanisms of disease. Effects on DMT on CD4+Th1 cells and related cytokine and signaling pathways are discussed in more detail...
October 18, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27758699/design-synthesis-and-molecular-docking-studies-of-new-potential-piperazine-derivatives-as-cognition-enhancers
#12
Chhanda C Danta, Poonam Piplani
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. Still there is not a drug candidate that can cure the cognitive deficits completely. OBJECTIVE: Series of novel piperazine derivatives have been designed, synthesized and evaluated for cognition enhancing activity...
October 14, 2016: 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
#13
Millet Treinin, Roger L Papke, Eran Nizri, Yael Ben-David, Tehila Mizrachi, Talma Brenner
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. 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 a7 nAChR subunit that assembles into a homomeric receptor having unusual properties...
August 29, 2016: 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
#14
Elanur Aydin, Şener Taşdemir, Fazıl Hacımüftüoğlu, Hasan Türkez
Thymol (THY), which is a monocyclic monoterpene, is one of the major constituent of the essential oils of thyme and origanum. To date, although various biological activities of THY have been demonstrated, its neurotoxicity has never been explored. We aimed to describe in vitro antiproliferative and/or cytotoxic properties (by 3-(4,5 dimetylthiazol-2-yl)-2,5 diphenlytetrazolium bromide (MTT) test), genotoxic damage potentials (by single cell gel electrophoresis (SCGE)) and oxidative effects (by total antioxidant capacity (TAC) and total oxidative stress (TOS) analysis) of THY...
August 23, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27554921/effect-of-mrjf4-on-c6-glioma-cells-proliferation-and-migration
#15
Marcella Reale, Jole Fiorito
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-kB signaling pathway, activity of nitric oxide synthases (NOS), metalloproteinases (MMPs), and membrane adhesion proteins were investigated...
August 23, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27550615/cholinergic-system-and-neuroinflammation-implication-in-multiple-sclerosis
#16
Maria Di Bari, Giovanni Di Pinto, Marcella Reale, Guadalupe Mengod, Ada Maria Tata
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 unknown, inflammation and autoimmunity are considered to be key players of the disease. 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...
August 22, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27514542/how-valid-is-placebo-in-the-indian-setting
#17
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 in 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...
August 10, 2016: 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
#18
Marcella Reale, Ada Maria Tata
The α7 nicotinic receptor consists of identical subunits and is one of the most abundant acetylcholine receptor 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. Its function is involved in the regulation of a range of activities such as classical excitatory neurotransmission in some brain regions, modulation of the release of several neurotransmitters, regulation of neurite outgrowth, and even neuronal survival/death...
July 29, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27439371/piroxicam-source-for-synthesis-of-central-nervous-system-cns-acting-drugs
#19
A S Saganuwan
The use of Central nervous system acting drugs in the management of new 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.
July 19, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27356627/synthesis-and-antioxidant-properties-of-novel-memantine-derivatives
#20
Ivana Cacciatore, Erika Fornasari, Lisa Marinelli, Antonio Di Stefano, Piera Eusepi, Hasan Turkez, Stefania Fulle, Ester Sara Di Filippo, Andrea Scarabeo
BACKGROUND: Medicinal chemistry approaches are presently under investigation to develop new multifunctional drugs able to 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...
June 25, 2016: Central Nervous System Agents in Medicinal Chemistry
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