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Naphthyl Tetronic Acids as Multi‐Target Inhibitors of Bacterial Peptidoglycan Biosynthesis
Author(s) -
Mansour Tarek S.,
Caufield Craig E.,
Rasmussen Beth,
Chopra Rajiv,
Krishnamurthy Girija,
Morris Koi M.,
Svenson Kristine,
Bard Joel,
Smeltzer Claudia,
Naughton Shaughnessy,
Antane Schuyler,
Yang Youjun,
Severin Anatoly,
Quagliato Dominick,
Petersen Peter J.,
Singh Guy
Publication year - 2007
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200700094
Subject(s) - peptidoglycan , biosynthesis , chemistry , biochemistry , enzyme , peptide , stereochemistry , ic50 , escherichia coli , combinatorial chemistry , in vitro , gene
A pathway screen targeting multiple muramyl peptide synthesis inhibitors identified the naphthyl tetronic acids series. Optimization of this series based on IC 50 , K d and MIC values led to potent inhibitors. Compound 5 h was co‐crystallized in the active site of E. coli Mur B.