Quantitative structure activity relationships studies of non-steroidal anti-inflammatory drugs: A review

被引：25

作者：

Asirvatham, Sahaya ^{[1
]}

Dhokchawle, Bharat V. ^{[1
]}

Tauro, Savita J. ^{[1
]}

机构：

[1] St John Inst Pharm & Res, Dept Pharmaceut Chem, Palghat 401404, Maharashtra, India

来源：

ARABIAN JOURNAL OF CHEMISTRY | 2019年 / 12卷 / 08期

关键词：

Inflammation; Nonsteroidal anti-inflammatory drugs; Quantitative Structure Activity Relationships; Lipophilicity; BIOLOGICAL EVALUATION; 5-LIPOXYGENASE INHIBITORS; ANTIMICROBIAL EVALUATION; DUAL INHIBITORS; QSAR ANALYSIS; DERIVATIVES; DESIGN; CYCLOOXYGENASE-2; ANALOGS; 3D-QSAR;

D O I：

10.1016/j.arabjc.2016.03.002

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Inflammation is a local response of mammalian tissues to injury due to any agent. It is body's defense mechanism in order to eliminate or limit the spread of injurious agent as well to remove the consequent necrosed cells and tissues. Inflammation, being a complex phenomenon involves a number of cellular mediators. Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most commonly used drugs worldwide. Different chemical moieties possess different pharmacological activities, although there are few common descriptors which all drugs should have for a given activity. Quantitative Structure Activity Relationships (QSAR) is a useful mean which maximizes the potency of identifying a new lead moiety. The interactions of drugs with their biological counterparts are determined by intermolecular forces, i.e. by hydrophobic, polar, electrostatic, and steric interactions. Several QSAR models have been studied and all have shown some common results. It was observed that functional groups which enhance the lipophilicity also enhanced the anti-inflammatory activity. NSAID's activity is highly related with the lipophilicity and hence depends on the log P value. (C) 2016 The Authors. Published by Elsevier B.V. on behalf of King Saud University.

引用

页码：3948 / 3962

页数：15

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