Monika I. Konaklieva
American University, USA
Title: Non-transpeptidase binding lactams active against Mycobacterium tuberculosis
Biography
Biography: Monika I. Konaklieva
Abstract
We have designed Non-transpeptidase binding lactams active against Mycobacterium tuberculosis, synthesized and tested a novel class of non-transpeptidase, β-lactamase resistant monocyclic β-lactams that carry an arylthio group at C4; these thio ethers exhibit inhibitory and cidal highly active against the serine beta-lactamase producing Mycobacterium tuberculosis H37Rv (Mtb). Some of the compounds have demonstrated minimal inhibitory concentration (MIC) as low as 6.25 µg/ml in 7H9 and 0.19 µg/ml in GAST. Preliminary investigations indicate that these compounds are cidal to both replicating and non-replicating persistent Mtb. These compounds are promising candidates for lead optimization and target identification studies which are currently underway.