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New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agents

Abstract : Starting from the analysis of the hypothetical binding mode of our previous furan-based hit (I), we successfully achieved our objective to replace the nitro moiety, leading to the disclosure of a new lead exhibiting a strong activity against MbtI. Our best candidate 1 h displayed a Ki of 8.8 µM and its antimycobacterial activity (MIC99 = 250 µM) is conceivably related to mycobactin biosynthesis inhibition. These results support the hypothesis that 5-phenylfuran-2-carboxylic derivatives are a promising class of MbtI inhibitors.
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Submitted on : Thursday, June 10, 2021 - 4:17:02 PM
Last modification on : Thursday, April 14, 2022 - 3:54:03 PM
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Laurent Chiarelli, Matteo Mori, Giangiacomo Beretta, Arianna Gelain, Elena Pini, et al.. New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agents. Journal of Enzyme Inhibition and Medicinal Chemistry, Informa Healthcare, 2019, 34 (1), pp.823-828. ⟨10.1080/14756366.2019.1589462⟩. ⟨pasteur-03257047⟩

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