Novel benzoic thiazolidin-4-one derivatives targeting DevR/DosR dormancy regulator of Mycobacterium tuberculosis

Journal of Molecular Structure(2022)

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摘要
•Synthesis of 33 new analogues of substituted benzoic thiazolidin-4-one.•Development of high throughput assay for screening DevR inhibitors in Mycobacterium tuberculosis.•Identification of N5, N6 and N11 as specific and non-toxic inhibitors of DevR interfering with the hypoxic viability of mycobacteria.•In silico docking analysis suggests N5, N6 and N11 binding to common pocket in C-terminal domain of DevR. The interaction of N5, N6 and N11 with DevR was experimentally confirmed using thermal shift assay.
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关键词
Thiazolidin-4-ones,2-iminothiazolidin-4-one,2-haloacetamide,DevR/DosR,Mycobacterium tuberculosis,Mycobacterium bovis BCG,Dormancy,Anti-DevR/DosR compounds
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