Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold

X Liang, CJ Lee, X Chen, HS Chung, D Zeng…

Index: Liang, Xiaofei; Lee, Chul-Jin; Chen, Xin; Chung, Hak Suk; Zeng, Daina; Raetz, Christian R.H.; Li, Yaoxian; Zhou, Pei; Toone, Eric J. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 2 p. 852 - 860

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Citation Number: 40

Abstract

Compounds inhibiting LpxC in the lipid A biosynthetic pathway are promising leads for novel antibiotics against multidrug-resistant Gram-negative pathogens. We report the syntheses and structural and biochemical characterizations of LpxC inhibitors based on a diphenyl- diacetylene (1, 4-diphenyl-1, 3-butadiyne) threonyl-hydroxamate scaffold. These studies provide a molecular interpretation for the differential antibiotic activities of compounds with ...