385405-50-5Relevant academic research and scientific papers
Synthesis and anti-inflammatory activity of some 3, 5-diaryl-2-pyrazoline derivatives
Khalil, Omneya M.,Refaat, Hanan M.
, p. 1581 - 1590 (2012/06/16)
Eleven new 3-(4-bromophenyl)-5-(4-flirorophenyl)-2-pyrazoline derivatives 4-9 and 11-15 were synthesized by using 1-(4-bromophenyl)-3-(4-fluorophenyl) prop-2-en-1-one (3). The newly synthesized compounds were evaluated for anti-inflammatory activity against carrageenan edema in albino rats at a dose of 10 mg/kg. All the compounds of this series showed promising anti-inflammatory activity. The most active compound of this series, 7 was found to be most potent, which has shown higher percentage of inhibition of edema than the standard drug indomethacin.
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.
