Heterocyclic methylsulfone hydroxamic acid LpxC inhibitors as Gram-negative antibacterial agents

Autor:	Lisa Mullins, Daniel P. Uccello, Justin I. Montgomery, Ye Che, John P. O'Donnell, Mark S. Plummer, Joseph A. Abramite, Seung Won Chung, Loren M. Price, Mark C. Noe, Laura A. McAllister, Rose Barham, Mark J. Mitton-Fry, Andrew P. Tomaras, Usa Reilly, Matthew Frank Brown, Jinshan M. Chen, Joseph Penzien, Carol A. Menard, Veerabahu Shanmugasundaram, Robert M. Oliver
Rok vydání:	2012
Předmět:	Gram-negative bacteria Klebsiella pneumoniae Clinical Biochemistry Pharmaceutical Science Microbial Sensitivity Tests Hydroxamic Acids Biochemistry Amidohydrolases Structure-Activity Relationship chemistry.chemical_compound Heterocyclic Compounds Gram-Negative Bacteria Drug Discovery Structure–activity relationship Sulfones Enzyme Inhibitors Molecular Biology chemistry.chemical_classification Hydroxamic acid biology Organic Chemistry biology.organism_classification Anti-Bacterial Agents Enzyme chemistry Pseudomonas aeruginosa Molecular Medicine Antibacterial activity Bacterial outer membrane Bacteria
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 22:6832-6838
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5698632622184881fc9d9e040335da17 https://doi.org/10.1016/j.bmcl.2012.09.058 Zobrazit plný text záznamu Full Text from ScienceDirect