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Current Organic Synthesis


ISSN (Print): 1570-1794
ISSN (Online): 1875-6271

Review Article

Advances in Synthesis, Derivatization and Bioactivity of Isatin: A Review

Author(s): Garima Chauhan*, Dharam Pal Pathak, Faraat Ali, Rubina Bhutani, Garima Kapoor and Shaik Khasimbi

Volume 18 , Issue 1 , 2021

Published on: 24 September, 2020

Page: [37 - 74] Pages: 38

DOI: 10.2174/1570179417666200924150907

Price: $65


Background: Isatin (IST) is a crucial pharmacologically active compound, chemically known as indole- 1H-2,3-dione. Development of different IST based analogues acquired significant awareness because of its pronounced therapeutic importance such as analgesic, anticancer, anti-inflammatory, antitubercular, antimicrobial, antifungal, antiviral (effective against SARS coronavirus 3C protease) and many other activities, and represents an important class of heterocyclic compounds that can be used as a precursor for the synthesis of many useful drugs.

Objective: Previously, many articles were reported on IST synthesis and its different pharmacological activities but herein, we mentioned 59 different synthesis schemes of several IST derivatives/hybrids derived from the substitution of the nitrogen, aromatic ring, the second and third position of IST along with most potent molecule among each of synthesized libraries with their structural activity relationship (SAR). Using these standardized approaches, several biologically important compounds were developed like sunitinib, nintedanib, indirubin, etc and several studies have been carried out nowadays to develop newer compounds having fewer side effects and also overcome the problem of resistance.

Conclusion: This report critically reviews the different strategies for the designs and synthesis of several IST based compounds having different biological activities with SAR, which can favour further investigation and modification for the development of new and more potent entities.

Keywords: Antitubercular, antiviral, anticancer, anticonvulsant, anti-inflammatory, analgesic, Isatin.

Graphical Abstract
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