728875-33-0Relevant academic research and scientific papers
ETHYNYLBENZENE DERIVATIVES
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Page/Page column 95; 98, (2012/03/26)
Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.
Syntheses, structures and antibiotic activities of LpxC inhibitors based on the diacetylene scaffold
Liang, Xiaofei,Lee, Chul-Jin,Chen, Xin,Chung, Hak Suk,Zeng, Daina,Raetz, Christian R.H.,Li, Yaoxian,Zhou, Pei,Toone, Eric J.
, p. 852 - 860 (2011/03/19)
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 a substituted distal phenyl ring as well as the absolute stereochemical requirement at the C2, but not C3, position of the threonyl group.
