A Concise Synthesis of Pyrrole-Based Drug Candidates from α-Hydroxyketones, 3-Oxobutanenitrile, and Anilines

A simple and concise three-component synthesis of a key pyrrole framework was developed from the reaction between α-hydroxyketones, oxoacetonitriles, and anilines. The synthesis was used to obtain several pyrrole-based drug candidates, including COX-2 selective NSAID, antituberculosis lead candidate...

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Bibliographic Details
Main Authors: Mengxin Xia, Mardi Santoso, Ziad Moussa, Zaher M. A. Judeh
Format: Article
Language:English
Published: MDPI AG 2023-01-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/28/3/1265
Description
Summary:A simple and concise three-component synthesis of a key pyrrole framework was developed from the reaction between α-hydroxyketones, oxoacetonitriles, and anilines. The synthesis was used to obtain several pyrrole-based drug candidates, including COX-2 selective NSAID, antituberculosis lead candidates BM212, BM521, and BM533, as well as several analogues. This route has potential to obtain diverse libraries of these pyrrole candidates in a concise manner to develop optimum lead compounds.
ISSN:1420-3049