Functionalized 3-amino-imidazo[1,2-a]pyridines: A novel class of drug-like Mycobacterium tuberculosis glutamine synthetase inhibitors
2009; Elsevier BV; Volume: 19; Issue: 16 Linguagem: Inglês
10.1016/j.bmcl.2009.06.045
ISSN1464-3405
AutoresLuke R. Odell, Mikael Nilsson, Johan Gising, Olof Lagerlund, Daniel Muthas, Anneli Nordqvist, Anders Karlén, Mats Larhed,
Tópico(s)Cancer therapeutics and mechanisms
Resumo3-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.
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