Trisubstituted imidazoles as Mycobacterium tuberculosis glutamine synthetase inhibitors.

ABSTRACT: Mycobacterium tuberculosis glutamine synthetase (MtGS) is a promising target for antituberculosis drug discovery. In a recent high-throughput screening study we identified several classes of MtGS inhibitors targeting the ATP-binding site. We now explore one of these classes, the 2-tert-butyl-4,5-diarylimidazoles, and present the design, synthesis, and X-ray crystallographic studies leading to the identification of MtGS inhibitors with submicromolar IC(50) values and promising antituberculosis MIC values.

SUBMITTER: Gising J 

PROVIDER: S-EPMC3381009 | biostudies-literature | 2012 Mar

REPOSITORIES: biostudies-literature