Importance of Pharmacophore in Designing Anticonvulsant Agents.

IF 2.7 4区 医学 Q3 NEUROSCIENCES
Amol Kale, Rajendra Kakde, Smita Pawar, Vishal Jagtap, Rahul Dorgude
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引用次数: 0

Abstract

Drug design is one of the critical aspects of the drug development process. The present review focused on different heterocyclic molecules having anticonvulsant activity with structural diversity and common pharmacophoric features. For the first time (1995), Dimmock and his team introduced specific arrangements of three important pharmacophores for anticonvulsant activity. These pharmacophores include two hydrophobic binding sites and one hydrogen binding site. After a few years (2012), Pandeya modified Dimmock's concept by adding one more pharmacophoric feature as an electron donor in the previously suggested pharmacophoric arrangement of the anticonvulsant. As a result, numerous scientists designed anticonvulsant drugs based on Dimmock's and Pandeya's concept. In addition, marketed anticonvulsant preparation containing Riluzole, Phenobarbital, Progabide, Ralitoline, etc., also holds the suggested pharmacophores by Dimmock and Pandeya's pharmacophoric concept. This review mainly focuses on the compilation of reported scientific literature in the last decade on the pharmacophoric features of different heterocyclic anticonvulsants, which will help develop new anticonvulsants.

药效团在抗惊厥药物设计中的重要性。
药物设计是药物开发过程中的关键环节之一。本文综述了具有结构多样性和共同药效特征的抗惊厥活性的不同杂环分子。1995年,Dimmock和他的团队首次介绍了抗惊厥活性的三种重要药效团的具体排列。这些药物载体包括两个疏水结合位点和一个氢结合位点。几年后(2012年),Pandeya修改了Dimmock的概念,在先前建议的抗惊厥药的药效安排中增加了一个作为电子供体的药效特征。结果,许多科学家根据Dimmock和Pandeya的概念设计了抗惊厥药物。此外,已上市的含有利鲁唑、苯巴比妥、普鲁比德、利利托林等的抗惊厥药物制剂也具有Dimmock和Pandeya的药效概念所建议的药效团。本文主要对近十年来各类杂环类抗惊厥药的药理特点进行综述,以期为开发新型抗惊厥药提供参考。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
5.10
自引率
3.30%
发文量
158
审稿时长
6-12 weeks
期刊介绍: Aims & Scope CNS & Neurological Disorders - Drug Targets aims to cover all the latest and outstanding developments on the medicinal chemistry, pharmacology, molecular biology, genomics and biochemistry of contemporary molecular targets involved in neurological and central nervous system (CNS) disorders e.g. disease specific proteins, receptors, enzymes, genes. CNS & Neurological Disorders - Drug Targets publishes guest edited thematic issues written by leaders in the field covering a range of current topics of CNS & neurological drug targets. The journal also accepts for publication original research articles, letters, reviews and drug clinical trial studies. As the discovery, identification, characterization and validation of novel human drug targets for neurological and CNS drug discovery continues to grow; this journal is essential reading for all pharmaceutical scientists involved in drug discovery and development.
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