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Title: Pyridone Methylsulfone Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative Infections

Abstract

The synthesis and biological activity of a new series of LpxC inhibitors represented by pyridone methylsulfone hydroxamate 2a is presented. Members of this series have improved solubility and free fraction when compared to compounds in the previously described biphenyl methylsulfone hydroxamate series, and they maintain superior Gram-negative antibacterial activity to comparator agents.

Authors:
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  1. (Pfizer)
Publication Date:
Research Org.:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Org.:
INDUSTRY
OSTI Identifier:
1038269
Resource Type:
Journal Article
Journal Name:
J. Med. Chem.
Additional Journal Information:
Journal Volume: 55; Journal Issue: (4) ; 02, 2012; Journal ID: ISSN 0022-2623
Country of Publication:
United States
Language:
ENGLISH
Subject:
59 BASIC BIOLOGICAL SCIENCES; 60 APPLIED LIFE SCIENCES; 37 INORGANIC, ORGANIC, PHYSICAL AND ANALYTICAL CHEMISTRY; ANTIMICROBIAL AGENTS; BACTERIA; INHIBITION; SOLUBILITY; SYNTHESIS

Citation Formats

Montgomery, Justin I., Brown, Matthew F., Reilly, Usa, Price, Loren M., Abramite, Joseph A., Arcari, Joel, Barham, Rose, Che, Ye, Chen, Jinshan Michael, Chung, Seung Won, Collantes, Elizabeth M., Desbonnet, Charlene, Doroski, Matthew, Doty, Jonathan, Engtrakul, Juntyma J., Harris, Thomas M., Huband, Michael, Knafels, John D., Leach, Karen L., Liu, Shenping, Marfat, Anthony, McAllister, Laura, McElroy, Eric, Menard, Carol A., Mitton-Fry, Mark, Mullins, Lisa, Noe, Mark C., O’Donnell, John, Oliver, Robert, Penzien, Joseph, Plummer, Mark, Shanmugasundaram, Veerabahu, Thoma, Christy, Tomaras, Andrew P., Uccello, Daniel P., Vaz, Alfin, and Wishka, Donn G. Pyridone Methylsulfone Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative Infections. United States: N. p., 2012. Web. doi:10.1021/jm2014875.
Montgomery, Justin I., Brown, Matthew F., Reilly, Usa, Price, Loren M., Abramite, Joseph A., Arcari, Joel, Barham, Rose, Che, Ye, Chen, Jinshan Michael, Chung, Seung Won, Collantes, Elizabeth M., Desbonnet, Charlene, Doroski, Matthew, Doty, Jonathan, Engtrakul, Juntyma J., Harris, Thomas M., Huband, Michael, Knafels, John D., Leach, Karen L., Liu, Shenping, Marfat, Anthony, McAllister, Laura, McElroy, Eric, Menard, Carol A., Mitton-Fry, Mark, Mullins, Lisa, Noe, Mark C., O’Donnell, John, Oliver, Robert, Penzien, Joseph, Plummer, Mark, Shanmugasundaram, Veerabahu, Thoma, Christy, Tomaras, Andrew P., Uccello, Daniel P., Vaz, Alfin, & Wishka, Donn G. Pyridone Methylsulfone Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative Infections. United States. doi:10.1021/jm2014875.
Montgomery, Justin I., Brown, Matthew F., Reilly, Usa, Price, Loren M., Abramite, Joseph A., Arcari, Joel, Barham, Rose, Che, Ye, Chen, Jinshan Michael, Chung, Seung Won, Collantes, Elizabeth M., Desbonnet, Charlene, Doroski, Matthew, Doty, Jonathan, Engtrakul, Juntyma J., Harris, Thomas M., Huband, Michael, Knafels, John D., Leach, Karen L., Liu, Shenping, Marfat, Anthony, McAllister, Laura, McElroy, Eric, Menard, Carol A., Mitton-Fry, Mark, Mullins, Lisa, Noe, Mark C., O’Donnell, John, Oliver, Robert, Penzien, Joseph, Plummer, Mark, Shanmugasundaram, Veerabahu, Thoma, Christy, Tomaras, Andrew P., Uccello, Daniel P., Vaz, Alfin, and Wishka, Donn G. Fri . "Pyridone Methylsulfone Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative Infections". United States. doi:10.1021/jm2014875.
@article{osti_1038269,
title = {Pyridone Methylsulfone Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative Infections},
author = {Montgomery, Justin I. and Brown, Matthew F. and Reilly, Usa and Price, Loren M. and Abramite, Joseph A. and Arcari, Joel and Barham, Rose and Che, Ye and Chen, Jinshan Michael and Chung, Seung Won and Collantes, Elizabeth M. and Desbonnet, Charlene and Doroski, Matthew and Doty, Jonathan and Engtrakul, Juntyma J. and Harris, Thomas M. and Huband, Michael and Knafels, John D. and Leach, Karen L. and Liu, Shenping and Marfat, Anthony and McAllister, Laura and McElroy, Eric and Menard, Carol A. and Mitton-Fry, Mark and Mullins, Lisa and Noe, Mark C. and O’Donnell, John and Oliver, Robert and Penzien, Joseph and Plummer, Mark and Shanmugasundaram, Veerabahu and Thoma, Christy and Tomaras, Andrew P. and Uccello, Daniel P. and Vaz, Alfin and Wishka, Donn G.},
abstractNote = {The synthesis and biological activity of a new series of LpxC inhibitors represented by pyridone methylsulfone hydroxamate 2a is presented. Members of this series have improved solubility and free fraction when compared to compounds in the previously described biphenyl methylsulfone hydroxamate series, and they maintain superior Gram-negative antibacterial activity to comparator agents.},
doi = {10.1021/jm2014875},
journal = {J. Med. Chem.},
issn = {0022-2623},
number = (4) ; 02, 2012,
volume = 55,
place = {United States},
year = {2012},
month = {11}
}