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Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors

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 Fa...

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Main 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.
Format: Article
Language:English
Published: 2017
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spelling my.uniten.dspace-35192017-10-27T07:02:36Z Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors 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. 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. 2017-10-27T06:55:22Z 2017-10-27T06:55:22Z 2014 Article 10.1515/epoly-2015-0017 en E-Polymers Volume 15, Issue 3, 1 May 2015, Pages 141-150
institution Universiti Tenaga Nasional
building UNITEN Library
collection Institutional Repository
continent Asia
country Malaysia
content_provider Universiti Tenaga Nasional
content_source UNITEN Institutional Repository
url_provider http://dspace.uniten.edu.my/
language English
description 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.
format Article
author 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.
spellingShingle 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.
Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors
author_facet 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.
author_sort Takhi, M.
title Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors
title_short Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors
title_full Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors
title_fullStr Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors
title_full_unstemmed Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors
title_sort discovery of azetidine based ene-amides as potent bacterial enoyl acp reductase (fabi) inhibitors
publishDate 2017
_version_ 1644493548614057984
score 13.211869

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