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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Review Article (Mini-Review)

Synthetic Strategies Towards Safer NSAIDs Through Prodrug Approach: A Review

Author(s): Komal Gupta, Pooja A Chawla* and Deepika Sharma

Volume 21 , Issue 15 , 2021

Published on: 31 December, 2020

Page: [2065 - 2102] Pages: 38

DOI: 10.2174/1389557521666201231140554

Price: $65

Abstract

Non-steroidal anti-inflammatory drugs (NSAIDs) are agents that are used for various properties such as analgesic activity, anti-inflammatory activity, antipyretic activity, etc. But this class of drugs is associated with different side effects such as dyspepsia, gastroduodenal ulcers, gastrointestinal (GI) bleeding and perforation. The prodrug approach is quite beneficial to curb these side effects. Prodrugs are the inactive compounds that, on metabolism get converted into an active metabolite exhibiting desired activities. Commonly used approaches for synthesizing prodrugs are amide, esters, and mutual prodrugs by suppressing the free carboxylic groups responsible for these side effects. In this review, different schemes reported for the synthesis of NSAIDs that are devoid of undesired side effects such as irritation to gastric mucosa, gastrotoxicity, and ulcerogenicity have been compiled. Docking studies and the structure-activity relationship of some compounds are also discussed. The paper shall help the researchers to understand the methods to expedite the synthesis by carrying out substitutions of various groups of the parent compound and establish the mechanism of action of these derivatives of masking the unwanted side effects.

Keywords: NSAIDs, Prodrugs, GI bleeding, GI ulcers, gastroprotective, anti-inflammatory, analgesic.

Graphical Abstract

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