Discovery of novel anti-tuberculosis agents with pyrrolo[1,2-a]quinoxaline-based scaffold

Bioorganic & Medicinal Chemistry Letters
Ting WangYoufu Luo

Abstract

A series of small molecules with novel pyrrolo[1,2-a]quinoxaline-based scaffold was designed via molecular hybridization of privileged agents active against Mycobacterium tuberculosis. Twenty-three compounds were synthesized and investigated for their antitubercular activities in vitro where ten compounds showed appreciable activities and moderate cytotoxicity. Compound 12g with MIC values of 5 μg/ml as a representative may possess better oral bioavailability and indicated high permeability by the parallel artificial membrane permeation assay of the blood-brain barrier (PAMPA-BBB). Further, the determination of enzyme inhibition and molecular docking study indicated that InhA may be the biological target of the active compounds. The results suggest the pyrrolo[1,2-a]quinoxaline hybrids as potential antitubercular leads for the development of new antitubercular agents.

Citations

Nov 5, 2020·Organic & Biomolecular Chemistry·Zhen YangYu Wei
May 28, 2021·Organic & Biomolecular Chemistry·Yali LiuPing Liu
Aug 28, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Marc MontanaPatrice Vanelle
Jan 8, 2022·Organic & Biomolecular Chemistry·Di HaoPing Liu

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