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Non-transpeptidase binding lactams active against Mycobacterium t | 32159
Journal of Pharmaceutical Care & Health Systems

Journal of Pharmaceutical Care & Health Systems
Open Access

ISSN: 2376-0419

+44 1300 500008

Non-transpeptidase binding lactams active against Mycobacterium tuberculosis


4th African Pharma Congress

June 20-21, 2016 Cape Town, South Africa

Monika I Konaklieva, Rostislav Kuskovsky, Kriti Arora, Helena I Boshoff and Clifton E Barry III

American University, USA
National Institute of Allergy and Infectious Diseases, USA

Scientific Tracks Abstracts: J Pharma Care Health Sys

Abstract :

We have designed Non-transpeptidase binding lactams active against Mycobacterium tuberculosis, synthesized and tested a novel class of non-transpeptidase, �?²-lactamase resistant monocyclic �?²-lactams that carry an arylthio group at C4; these thio ethers exhibit inhibitory and cidal highly active against the serine beta-lactamase producing H37Rv (Mtb). Some of the compounds have demonstrated minimal inhibitory concentration (MIC) as low as 6.25 �?¼g/ml in 7H9 and 0.19 �?¼g/ml in GAST. Preliminary investigations indicate that these compounds are cidal to both replicating and nonreplicating persistent Mtb. These compounds are promising candidates for lead optimization and target identification studies which are currently underway.

Biography :

Monika I Konaklieva has obtained her Doctoral degree in Organic Synthetic Chemistry from State University of New York at Buffalo (1997). She is currently an Associate Professor in the Department of Chemistry, American University, Washington, DC. In 2007, she spent her sabbatical leave at the Tuberculosis Research Section, LCID, NIAID, NIH. Her research focuses on the synthesis and evaluation of new antibacterial, neuroprotective and anticancer agents, as well as development of efficient and environmetally friendly synthetic approaches for their preparation.

Email: mkonak@american.edu

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