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Mini-Reviews in Medicinal Chemistry


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

Mini-Review Article

Recent Progress of Bioactivities, Mechanisms of Action, Total Synthesis, Structural Modifications and Structure-activity Relationships of Indole Derivatives: A Review

Author(s): Tianze Li and Hui Xu*

Volume 22, Issue 21, 2022

Published on: 31 May, 2022

Page: [2702 - 2725] Pages: 24

DOI: 10.2174/1389557522666220330123538

Price: $65


Indole (2,3-benzopyrrole) containing a pyrrolyl ring possesses the characteristic of electron- rich aromatic compounds. Indole occurs in the oil of jasmine and cloves and coal tar. Additionally, it is also present as a putrefaction product from animals' intestines. Notably, indole and its derivatives exhibit a wide range of biological properties, such as anti-Alzheimer’s disease, anti-cancer, antibacterial, anti-inflammatory, anti-human immunodeficiency virus (HIV), anti-diabetic, antituberculosis, anti-oxidant, anti-coronavirus, and antifungal activities. In this mini-review, recent advances in biological activities, mechanisms of action, total synthesis, structural modifications, and structure-activity relationships of indole and its derivatives from 2018 to 2020 are described. We hope the present paper can pave the way for future design, development, and application of indole derivatives as potent drugs.

Keywords: Indole, indole derivatives, biological activity, mechanism of action, total synthesis, structural modification, structural- activity relationship.

Graphical Abstract
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