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Central Nervous System Agents in Medicinal Chemistry

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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
https://www.readbyqxmd.com/read/27160716/understanding-the-metabolic-consequences-of-human-arylsulfatase-a-deficiency-through-a-computational-systems-biology-study
#16
Y Echeverri Olga, A Salazar Diego, Alexander Rodriguez-Lopez, González Janneth, J Almeciga-Diaz Carlos, A Barrera Luis
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. Mutations affecting ARSA function lead to the neurodegenerative disease Metachromatic Leukodystrophy. This disease is characterized by accumulation of sulfatide within the band of myelin affecting its functionality...
May 10, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27149992/astrocyte-s-rage-more-than-just-a-question-of-mood
#17
Rodrigo E González-Reyes, María Graciela Rubiano
Adequate function of the nervous system depends on the balance of glia-neuron 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...
May 4, 2016: 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
#18
Quankun Zhuang, Cailing Dai, Linglong Yang, Huimin Wen, Hongyun Wang, Xiaoxue Jiang, Yuyang Zhang
Anandamide system is mainly made up of cannabinoid receptors, their endogenous ligands and some related enzymes. Activation of the system mediates various molecular events, thereafter leading to vasodilation, bradycardia and anti-inflammation. The stimulated cannabinoid receptors may take part in protection of endothelial cells from injury and therefore can be potential targets in therapy for some diseases, especially cardio or cerebral vascular disturbances. Cerebral ischemia is a deadly disease that modern people have to face and will probably face for a long period of time...
May 3, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27121380/physiological-targets-for-the-treatment-of-diabetic-encephalopathy
#19
Lucas Lima Vieira, Rafaela Gomes de Lima Soares, Stela Mirla da Silva Felipe, Felipe Carmo de Moura, Gerly Anne de Castro Brito, Christina Pacheco, Paula Matias Soares
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...
April 28, 2016: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27063392/drug-design-strategies-for-the-discovery-of-novel-anticonvulsants-concerned-with-four-site-binding-pharmacophoric-model-studies
#20
Deepak K Jain, Avineesh Singh, Vijay K Patel, Ravichandran Veerasamy, Navneet Aggarwal, Harish Rajak
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. Semicarbazones have been developed as versatile anticonvulsant pharmacophore. It has displayed potent anticonvulsant effect in a wide variety of preclinical anticonvulsant models...
April 11, 2016: Central Nervous System Agents in Medicinal Chemistry
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