苯妥英类衍生物的合成及其中枢神经系统活性。

Rahul Chauhan, Shwetank Verma, Alankar Shrivasatava
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引用次数: 0

摘要

背景合成了苯妥英与各种苯胺类化合物的偶联衍生物。使用不同的软件程序评估合成的衍生物的不同物理化学参数以及Log P值,以发现其穿越血脑屏障的能力。采用不同模型评价其抗焦虑、骨骼肌松弛剂、抗惊厥等药理活性。目的合成新的苯妥英钠衍生物,并对其不同性质进行评价,以预测其中枢神经系统活性。以氯乙酰化合成的药物为原料,加入不同的苯胺,采用不同的方法对其中枢神经系统活性进行评价。方法以苯妥英为原料,经氯乙酰化反应合成苯妥英,然后加入不同的取代苯胺,用不同的模型评价苯妥英的抗焦虑活性、肌肉松弛活性和抗惊厥活性。结果合成了苯妥英多个衍生物,并对各种理化参数进行了优化,结果表明含氯基团的化合物C2和C5与标准药物安定相比具有显著的潜力,研究了苯妥英新衍生物的抗焦虑和骨骼肌松弛活性。这些化合物被高效合成,并通过分子对接研究进行了描述。这些化合物相对于标准药物也表现出轻度至中度的相似性。合成的药物有可能被进一步优化,以产生新的支架来治疗各种中枢神经系统疾病。
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Synthesis and CNS Activity of Phenytoin derivatives.
BACKGROUND The derivatives of Phenytoin conjugated with various anilines were synthesized. The synthesized derivatives were evaluated for different physicochemical parameters along with Log P values using different software programs to discover its ability to cross the blood brain barrier. The pharmacological activities such as antianxiety, skeletal muscle relaxant and anticonvulsant were evaluated by using different models. OBJECTIVE The new Phenytoin derivatives were synthesized and evaluated for different properties to predict its CNS activity. The drugs synthesized by chloroacetylation and then different aniline were added into it. The compounds were evaluated for their different CNS activity by using different methods. METHOD The compounds were synthesized by firstly chloroacetylating the phenytoin and then different substituted aniline were added into it. The compounds were evaluated for antianxiety activity, Muscle relaxant activity and anticonvulsant activity by using different models. RESULT The number of derivatives of Phenytoin was synthesized and various physicochemical parameters were optimized which reveal that the compound containing chloro group such as C2 and C5 exhibited significant potential when compared with the standard drug Diazepam. CONCLUSION It was portrayed that the synthesis, computational studies and evaluation of anticonvulsant, antianxiety and skeletal muscle relaxant activity of new Phenytoin derivatives were carried out. The compounds were productively synthesized and portrayed by molecular docking studies. The compounds also exhibit mild to moderate similarity with respect to standard drug. The synthesized drugs have the potential to be optimized further to engender new scaffolds to treat various CNS disorders.
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来源期刊
Central nervous system agents in medicinal chemistry
Central nervous system agents in medicinal chemistry Psychology-Neuropsychology and Physiological Psychology
CiteScore
2.10
自引率
0.00%
发文量
21
期刊介绍: Central Nervous System Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new central nervous system agents. Containing a series of timely in-depth reviews written by leaders in the field covering a range of current topics, Central Nervous System Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in the field.
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