Biochemical and microbiological evaluation of N-aryl urea derivatives against mycobacteria and mycobacterial hydrolases.

ABSTRACT: A focused library of 24 N-aryl urea derivatives was prepared and evaluated against serine esterases of Mycobacterium tuberculosis (Mtb) Rv3802c and Mtb Ag85C. The members of the library were evaluated for both selectivity and mode of inhibition. Furan-based urea derivative 6c was found to be the most potent non-covalent inhibitor of Rv3802c with a K _i value of 5.2 ± 0.7 μM. On the other hand, triazole-based ureas 10a and 10b selectively inhibited Ag85C irreversibly with a k _inact/K _i value of 2.3 ± 0.3 and 5.5 ± 0.4 × 10^-3 μM^-1 min^-1, respectively. The library was also evaluated for minimum inhibitory concentration (MIC) against two strains of Mtb,

SUBMITTER: Vartak A 

PROVIDER: S-EPMC6677023 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature