93320-29-7Relevant academic research and scientific papers
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.
Microwave assisted synthesis of 2-pyrazolines
Paul, Satya
, p. 1279 - 1282 (2007/10/03)
A simple and efficient method has been developed for the rapid synthesis of 1-acetyl-3, 5-diaryl-2-pyrazolines 2 from chalcones 1 and hydrazine hydrate in unmodified domestic microwave oven in unsealed borosil vessels using acetic acid as energy transfer medium. Rate enhancement with improved yield, a characteristic of the synthesis under microwave irradiation has been observed in the present paper. The compounds synthesised have been characterised and compared with samples prepared by thermal methods.
