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

Autor:	Bodo Scheiper, Bernard Pessegue, Axel Ganzhorn, Christoph Pöverlein, Cédric Couturier, Sandra Silve, Eric Bacqué, Armin Bauer, Anil Nair, Renaud Morales, Sylvie Llopart, Sophie Lagrange
Rok vydání:	2015
Předmět:	Models Molecular Tuberculosis Stereochemistry High-throughput screening Clinical Biochemistry Antitubercular Agents Pharmaceutical Science Crystallography X-Ray Heterocyclic Compounds 4 or More Rings Biochemistry Mycobacterium tuberculosis Glutamate-Ammonia Ligase Glutamine synthetase Drug Discovery medicine Enzyme Inhibitors Molecular Biology Biological evaluation Molecular Structure biology Chemistry Organic Chemistry Imidazoles biology.organism_classification medicine.disease High-Throughput Screening Assays Crystallography Pyrazines Molecular Medicine Whole cell
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 25:1455-1459
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ae9b3cfa07ea339bf3443a7b1877766 https://doi.org/10.1016/j.bmcl.2015.02.035 Zobrazit plný text záznamu Full Text from ScienceDirect