National Center for
4XYC: Nanomolar Inhibitors Of Mycobacterium Tuberculosis Glutamine Synthetase 1: Synthesis, Biological Evaluation And X-ray Crystallographic Studies
Nanomolar inhibitors of Mycobacterium tuberculosis glutamine synthetase 1: Synthesis, biological evaluation and X-ray crystallographic studies
Bioorg. Med. Chem. Lett. (2015) 25 p.1455-1459
A series of imidazo[1,2-a]indeno[1,2-e]pyrazin-4-ones that potently inhibit M. tuberculosis glutamine synthetase (GlnA1) has been identified by high throughput screening. Exploration of this series was performed owing to a short chemistry program. Despite possibly nanomolar inhibitions, none of these compounds was active on whole cell Mtb, suggesting that GlnA1 may not be a suitable target to find new anti-tubercular drugs.