Title

Heterocyclic Methylsulfone Hydroxamic Acid LpxC Inhibitors as Gram-Negative Antibacterial Agents

Document Type

Article

Publication Date

2012

Publication Title

Bioorganic & Medicinal Chemistry Letters

Volume Number

22

Issue Number

22

DOI

10.1016/j.bmcl.2012.09.058

Abstract

The synthesis and antibacterial activity of heterocyclic methylsulfone hydroxamates is presented. Compounds in this series are potent inhibitors of the LpxC enzyme, a key enzyme involved in the production of lipopolysaccharide (LPS) found in the outer membrane of Gram-negative bacteria. SAR evaluation of compounds in this series revealed analogs with potent antibacterial activity against challenging Gram-negative species such as Pseudomonas aeruginosa and Klebsiella pneumoniae.

ISSN

0960-894X

First Page

6832

Last Page

6838

Link Out URL

https://doi.org/10.1016/j.bmcl.2012.09.058

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