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• W1201151557 abstract "Tuberculosis (TB) is a major global health problem, and new drug targets and scaffolds need to be identified to combat the emergence of drug resistant TB. The nitroimidazooxazine PA-824 represents a new class of bio-reductive drug to treat TB. In this study we report a 2-nitroimidazooxazine derivative with modification at the C-7 position that exhibited better activity than PA-824 against Mycobacterium tuberculosis (Mtb) H37Rv strain in vitro. From 7a as a key intermediate, we functionalized with benzyl ether (8), phenyl ether (9), benzyl carbonate (10) and benzyl carbamate (11). Among the 23 compounds produced, 8a-R (MIC=0.078 μM) with trifluoromethoxy benzyl group was 5-fold more potent than PA-824 (MIC=0.390 μM) in the in vitro assays against the wild-type Mtb, and the phenyl ether compound 9g-R (MIC=0.050 μM) exhibited the most potent antimycobacterial activity." @default.
• W1201151557 created "2016-06-24" @default.
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• W1201151557 date "2015-09-01" @default.
• W1201151557 modified "2023-09-27" @default.
• W1201151557 title "Synthesis and anti-tubercular activity of 2-nitroimidazooxazines with modification at the C-7 position as PA-824 analogs" @default.
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• W1201151557 doi "https://doi.org/10.1016/j.bmcl.2015.06.060" @default.
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