Quinoxaline Moiety: A Potential Scaffold against Mycobacterium tuberculosis.

Marc Montana,Omar Khoumeri,Patrice Vanelle,Vincent Montero

doi:10.3390/molecules26164742

Abstract

Background. The past decades have seen numerous efforts to develop new antitubercular agents. Currently, the available regimens are lengthy, only partially effective, and associated with high rates of adverse events. The challenge is therefore to develop new agents with faster and more efficient action. The versatile quinoxaline ring possesses a broad spectrum of pharmacological activities, ensuring considerable attention to it in the field of medicinal chemistry. Objectives. In continuation of our program on the pharmacological activity of quinoxaline derivatives, this review focuses on potential antimycobacterial activity of recent quinoxaline derivatives and discusses their structure—activity relationship for designing new analogs with improved activity. Methods. The review compiles recent studies published between January 2011 and April 2021. Results. The final total of 23 studies were examined. Conclusions. Data from studies of quinoxaline and quinoxaline 1,4-di-N-oxide derivatives highlight that specific derivatives show encouraging perspectives in the treatment of Mycobacterium tuberculosis and the recent growing interest for these scaffolds. These interesting results warrant further investigation, which may allow identification of novel antitubercular candidates based on this scaffold.

Highlights

IntroductionTreatment of drug-susceptible active tuberculosis consists of a standard 6-month regimen of four antimicrobials (usually isoniazid, rifampin, pyrazinamide, and ethambutol) [2,3]
This review highlights the growing interest in the development of compounds bearing This review highlights the growing interest in the development of compounds beara quinoxaline moiety for antimycobacterial treatment, some of these compounds having ing a quinoxaline moiety for antimycobacterial treatment, some of these compounds havreached the preclinical evaluation phase
Both quinoxaline and ing reached the preclinical evaluation phase. Both quinoxaquinoxaline-1,4-di-N-oxides with a variety of substituents in positions 2, 3, 6, and 7 showed line and quinoxaline-1,4-di-N-oxides with a variety of substituents in positions 2, 3, 6, and anti-TB activity

Summary

Introduction

Treatment of drug-susceptible active tuberculosis consists of a standard 6-month regimen of four antimicrobials (usually isoniazid, rifampin, pyrazinamide, and ethambutol) [2,3]. These regimens are lengthy, only partially effective, and associated with high rates of adverse events. The challenge is to develop new agents with faster and more efficient action. In continuation of our program on the pharmacological activity of quinoxaline derivatives, this review focuses on potential antimycobacterial activity of recent quinoxaline derivatives and discusses their structure—activity relationship for designing new analogs with improved activity. The review compiles recent studies published between January 2011 and April 2021.

Methods

Results

Discussion

Conclusion