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

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机构： [a]Department of Medicinal Chemistry, Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, West China School of Pharmacy, and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041, China [b]Institute of Physical Science and Information Technology, Anhui University, Hefei 230039, China [c]State Key Laboratory of Respiratory Disease, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510000, China

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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. Copyright © 2018 Elsevier Ltd. All rights reserved.

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出版当年[2018]版：

大类 | 3 区医学

小类 | 3 区药物化学 3 区有机化学

最新[2023]版：

大类 | 4 区医学

小类 | 2 区有机化学 4 区药物化学

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第一作者机构： [a]Department of Medicinal Chemistry, Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, West China School of Pharmacy, and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041, China

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