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Pharma & Clinical Pharmacy Congress 2016
November 07-09, 2016
Volume 5 Issue 4(Suppl)
Clin Pharmacol Biopharm
ISSN: 2167-065X CPB, an open access journal
conferenceseries
.com
November 07-09, 2016 Las Vegas, Nevada, USA
4
th
International
Pharma & Clinical Pharmacy Congress
Monika I Konaklieva et al., Clin Pharmacol Biopharm 2016, 5:4(Suppl)
http://dx.doi.org/10.4172/2167-065X.C1.023Non-transpeptidase binding aryl-thioether β-lactams active against
Mycobacterium tuberculosis
Monika I Konaklieva
1
, Rostislav Kuskovsky
1
and Kriti Arora
2
1
American University, USA
2
National Institute of Allergy and Infectious Diseases, USA
W
e have designed, synthesized and tested a novel class of non-transpeptidase, β-lactamase resistant monocyclic β-lactams
that carry an aryl-thio group at C4. These thio-ethers exhibit inhibitory and cidal activity against serine β-lactamase
producing
Mycobacterium tuberculosis
wild type strain (Mtb). Some of the compounds have demonstrated minimal inhibitory
concentration (MIC) as low as 6.25 µg/ml in 7H9 and 1.5 µg/ml in GAST. Our investigations indicate that these compounds
are cidal to both replicating and non-replicating persistent Mtb. These compounds have also shown activity against multi-drug
resistant strains of
M. tuberculosis.
Therefore, they are promising candidates for lead discovery. Mechanism of action and target
identification studies which are currently underway.
Biography
Monika I Konaklieva has completed her PhD in Chemistry from SUNY Buffalo in the year 1997. She was a Visiting Professor in Medicinal Chemistry at Midwestern
University, Chicago, Illinois. She is currently an Associate Professor at American University. She has published more than 40 papers in reputed journals and has
been serving as an Editorial Board Member of several Chemistry journals publishing in the areas of Organic and Medicinal Chemistry.
mkonak@american.edu