Please use this identifier to cite or link to this item: http://dspace.uniten.edu.my/jspui/handle/123456789/3519
Title: Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors
Authors: Takhi, M. 
Sreenivas, K. 
Reddy, C.K. 
Munikumar, M. 
Praveena, K. 
Sudheer, P. 
Rao, B.N.V.M. 
Ramakanth, G. 
Sivaranjani, J. 
Mulik, S. 
Reddy, Y.R. 
Narasimha Rao, K. 
Pallavi, R. 
Lakshminarasimhan, A. 
Panigrahi, S.K. 
Antony, T. 
Abdullah, I. 
Lee, Y.K. 
Ramachandra, M. 
Yusof, R. 
Rahman, N.A. 
Subramanya, H. 
Issue Date: 2014
Journal: E-Polymers Volume 15, Issue 3, 1 May 2015, Pages 141-150 
Abstract: A novel and potent series of ene-amides featuring azetidines has been developed as FabI inhibitors active against drug resistant Gram-positive pathogens particularly staphylococcal organisms. Most of the compounds from the series possessed excellent biochemical inhibition of Staphylococcus aureus FabI enzyme and whole cell activity against clinically relevant MRSA, MSSA and MRSE organisms which are responsible for significant morbidity and mortality in community as well as hospital settings. The binding mode of one of the leads, AEA16, in Escherichia coli FabI enzyme was determined unambiguously using X-ray crystallography. The lead compounds displayed good metabolic stability in mice liver microsomes and pharmacokinetic profile in mice. The in vivo efficacy of lead AEA16 has been demonstrated in a lethal murine systemic infection model. © 2014 Published by Elsevier Masson SAS.
DOI: 10.1515/epoly-2015-0017
Appears in Collections:COE Scholarly Publication

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