Nanomolar inhibitors of Mycobacterium tuberculosis glutamine synthetase 1: synthesis, biological evaluation and X-ray crystallographic studies

Bioorganic & Medicinal Chemistry Letters
Cédric CouturierEric Bacqué

Abstract

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.

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Citations

Jun 8, 2017·The Journal of Physical Chemistry. B·Cátia MoreiraPedro A Fernandes
Jul 18, 2020·Journal of Biological Inorganic Chemistry : JBIC : a Publication of the Society of Biological Inorganic Chemistry·Eduardo H S SousaJosé J G Moura
Aug 12, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Cátia MoreiraPedro A Fernandes
Nov 4, 2020·Biomolecules·Brittany L Carroll, Jun Liu

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