Indol-3-ylglyoxylamide as Privileged Scaffold in Medicinal Chemistry

Author:

Barresi Elisabetta1ORCID,Robello Marco2,Baglini Emma1,Poggetti Valeria1,Viviano Monica3ORCID,Salerno Silvia1ORCID,Da Settimo Federico1ORCID,Taliani Sabrina1ORCID

Affiliation:

1. Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy

2. Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), National Institutes of Health, 9000 Rockville Pike, Bethesda, MD 20892, USA

3. Department of Pharmacy, University of Salerno, 84084 Fisciano, Italy

Abstract

In recent years, indolylglyoxylamide-based derivatives have received much attention due to their application in drug design and discovery, leading to the development of a wide array of compounds that have shown a variety of pharmacological activities. Combining the indole nucleus, already validated as a “privileged structure,” with the glyoxylamide function allowed for an excellent template to be obtained that is suitable to a great number of structural modifications aimed at permitting interaction with specific molecular targets and producing desirable therapeutic effects. The present review provides insight into how medicinal chemists have elegantly exploited the indolylglyoxylamide moiety to obtain potentially useful drugs, with a particular focus on compounds exhibiting activity in in vivo models or reaching clinical trials. All in all, this information provides exciting new perspectives on existing data that can be useful in further design of indolylglyoxylamide-based molecules with interesting pharmacological profiles. The aim of this report is to present an update of collection data dealing with the employment of this moiety in the rational design of compounds that are able to interact with a specific target, referring to the last 20 years.

Funder

University of Pisa

Publisher

MDPI AG

Subject

Drug Discovery,Pharmaceutical Science,Molecular Medicine

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