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Heterocyclic methylsulfone hydroxamic acid LpxC inhibitors as Gram-negative antibacterial agents |
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| Authors: | Laura A McAllister Justin I Montgomery Joseph A Abramite Usa Reilly Matthew F Brown Jinshan M Chen Rose A Barham Ye Che Seung Won Chung Carol A Menard Mark Mitton-Fry Lisa M Mullins Mark C Noe John P O’Donnell Robert M Oliver Joseph B Penzien Mark Plummer Loren M Price Veerabahu Shanmugasundaram Andrew P Tomaras Daniel P Uccello |
| Institution: | Pfizer Worldwide Research and Development, 445 Eastern Point Road, Groton, CT 06340, USA |
| 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. |
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