132577-30-1Relevant articles and documents
Design, synthesis, and structure-activity relationships of pyrazole derivatives as potential FabH inhibitors
Lv, Peng-Cheng,Sun, Juan,Luo, Yin,Yang, Ying,Zhu, Hai-Liang
scheme or table, p. 4657 - 4660 (2010/09/16)
Fatty acid biosynthesis is essential for bacterial survival. FabH, β-ketoacyl-acyl carrier protein (ACP) synthase III, is a particularly attractive target, since it is central to the initiation of fatty acid biosynthesis and is highly conserved among Gram-positive and -negative bacteria. Fifty-six 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives were synthesized and developed as potent inhibitors of FabH. This inhibitor class demonstrates strong antibacterial activity. Escherichia coli FabH inhibitory assay and docking simulation indicated that the compounds 1-(5-(4-fluorophenyl)- 3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (12) and 1-(5-(4-chlorophenyl)-3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone (13) were potent inhibitors of E. coli FabH.
Synthesis of some 1-acetyl-3,5-diaryl-2-pyrazoline derivatives and their antimicrobial activities
Safak,Tayhan,Sarac,Yulug
, p. 571 - 574 (2007/10/02)
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