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8-Pyrrole-benzothiazinones non-covalent inhibitors of DprE1 from Mycobacterium tuberculosis.
분류 ADME 조회 1365
발행년도 2015 등록일 2015-09-26
출처 Antimicrob Agents Chemother (바로가기)
8-nitrobenzothiazinones, such as BTZ043 and PBTZ169, inhibit decaprenylphosphoryl-beta-D-ribose 2' -oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro. SAR studies revealed the 8-nitro group of the BTZ scaffold to be crucial for the mechanism of action, which involves formation of a semi-mercaptal bond with Cys387 in the active site of DprE1. To date, substitution of the 8-nitro group has led to extensive loss of antimycobacterial activity.
 
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