title: Synthesis and anti-inflammatory activity of new N-acyl-2-pyrazolines bearing homologous alkyloxy side chains.
abstract: A series of new pyrazoline derivatives (1a-2h) equipped with N-acyl arms and homologous alkyloxy side chains were synthesized and characterized on the basis of spectroscopic data and microanalysis. All the synthesized compounds were screened for their in-vitro anti-inflammatory activity to examine the effect of alkyloxy side chain length on activity. Compounds with odd number of carbons in alkyloxy side chain showed better activity as compared to even ones. Compound 2c (96% inhibition, IC(50) = 173.06 ± 2.312 mM) was found to be the most active compound of the series with better activity than the standard (Indomethacine, 92% inhibition, IC(50) = 273.12 ± 2.33 mM). Compound 1a (86%, IC(50) = 296.16 ± 2.091 mM) was the second best with comparable activity to the standard drug. However, the other compounds of series showed moderate to low activity. Interestingly, parallel cytotoxicity studies of compounds 1a-2h against PC-3 cell line revealed either no or very low cytotoxicity. The study may contribute in developing useful alternatives to presently used NSAIDs with harmful gastric effects due to direct cytotoxicity.
authors.forename: Asghar
authors.initials: A
authors.lastname: Abbas
authors.forename: Muhammad Moazzam
authors.initials: MM
authors.lastname: Naseer
mesh_terms: D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009504:Neutrophils / Q000187:drug effects; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000893:Anti-Inflammatory Agents; D011720:Pyrazoles