Synthetic approaches to potent heterocyclic inhibitors of tuberculosis: A decade review

Abstract

Tuberculosis (TB) continues to be a significant global health concern with about 1.5 million deaths annually. Despite efforts to develop more efficient vaccines, reliable diagnostics, and chemotherapeutics, tuberculosis has become a concern to world health due to HIV, the rapid growth of bacteria that are resistant to treatment, and the recently introduced COVID-19 pandemic. As is well known, advances in synthetic organic chemistry have historically enabled the production of important life-saving medications that have had a tremendous impact on patients’ lives and health all over the world. Small-molecule research as a novel chemical entity for a specific disease target offers in-depth knowledge and potential therapeutic targets. In this viewpoint, we concentrated on the synthesis of a number of heterocycles reported in the previous decade and the screening of their inhibitory action against diverse strains of Mycobacterium tuberculosis. These findings offer specific details on the structure-based activity of several heterocyclic scaffolds backed by their in vitro tests as a promising class of antitubercular medicines, which will be further useful to build effective treatments to prevent this terrible illness.

Ionic liquid‐supported copper‐catalyzed synthesis of 2H‐indazoles under microwave irradiation

“…Maintaining our pursuit of investigating the possible uses of bioactive compounds produced via a sustainable route for therapeutic application [56][57][58][59][60][61], herein, we report the ionic liquid-supported copper-catalyzed synthesis of 2H-indazoles under microwaves through the sequential formation of C-N and N-N bonds. The synthetic methods reported in this article include comprehensive details on the formation of the ionic liquid-supported copper catalyst as well as its catalytic application for the preparation of 2H-indazoles.…”

In Silico Design and Investigation of Novel Thiazetidine Derivatives as Potent Inhibitors of PrpR in Mycobacterium tuberculosis

“…Moreover, we have recently reported a detailed overview on the synthetic approaches to potent heterocyclic inhibitors of tuberculosis. [28] With respect to our ongoing methodology for the generation of bioactive scaffolds employing various computational techniques starting from 2-aminopyridine, [29] we have utilized a number of in-silico experiments including molecular docking and dynamic simulations, to discover the potential inhibitors of Mtb protein PrpR. Added to the above, ADMET and in-silico activity prediction also provide compounds' permeability and bioavailability evaluations which are key components in the drug design process.…”

“…The Lipinski rule of five has furthermore been applied to identify therapeutic interactions which are reliable and effective. Moreover, we have recently reported a detailed overview on the synthetic approaches to potent heterocyclic inhibitors of tuberculosis [28] . With respect to our ongoing methodology for the generation of bioactive scaffolds employing various computational techniques starting from 2‐aminopyridine, [29] we have utilized a number of in‐silico experiments including molecular docking and dynamic simulations, to discover the potential inhibitors of Mtb protein PrpR.…”