Functionalized 3-amino-imidazo[1,2-a]pyridines: A novel class of drug-like Mycobacterium tuberculosis glutamine synthetase inhibitors
2009 (English)In: Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, E-ISSN 1464-3405, Vol. 19, no 16, 4790-4793 p.Article in journal (Refereed) Published
3-Amino-imidazo[1,2-a]pyridines have been identified as a novel class of Mycobacterium tuberculosis glutamine synthetase inhibitors. Moreover, these compounds represent the first drug-like inhibitors of this enzyme. A series of compounds exploring structural diversity in the pyridine and phenyl rings have been synthesized and biologically evaluated. Compound 4n was found to be the most potent inhibitor (IC50 = 0.38 ± 0.02 μM). This compound was significantly more potent than the known inhibitors, L-methionine-SR-sulfoximine and phosphinothricin.
Place, publisher, year, edition, pages
2009. Vol. 19, no 16, 4790-4793 p.
Mycobacterium tuberculosis, Glutamine synthetase inhibitors, Microwave, 3-Aminoimidazo[1, 2-a]pyridine
IdentifiersURN: urn:nbn:se:uu:diva-100360DOI: 10.1016/j.bmcl.2009.06.045ISI: 000268358800057PubMedID: 19560924OAI: oai:DiVA.org:uu-100360DiVA: diva2:210171