Synthesis of 2-[5,6-diphenyl-3(2H)-pyridazinone-2-yl]acetamide and 3-[5,6-diphenyl-3(2H)-pyridazinone-2-yl]propanamide derivatives as analgesic and anti-inflammatory agents


DOĞRUER D. S. , ÜNLÜ S. , Küpeli E., Banogǧlu E., ŞAHİN M. G.

Turkish Journal of Pharmaceutical Sciences, vol.4, no.2, pp.57-70, 2007 (Journal Indexed in SCI Expanded) identifier

  • Publication Type: Article / Article
  • Volume: 4 Issue: 2
  • Publication Date: 2007
  • Title of Journal : Turkish Journal of Pharmaceutical Sciences
  • Page Numbers: pp.57-70

Abstract

In this study, new sixteen 2- [5,6-diphenyl-3(2H)-pyridazinone-2-yl ] acetamide and 3- [5,6-diphenyl-3(2H)-pyridazinone-2-yl ] propanamide derivatives were synthesized and their in vivo analgesic and anti-inflammatory activities were tested in mice. Propanamide derivatives were found more potent than acetamide derivatives in terms of anti-inflammatory activity. The compound 8e which is a propanamide derivative exhibited higher analgesic and anti-inflammatory activities than other synthesized compounds and did not cause any gastric lesions and bleeding in stomachs of tested animals. Inhibitory activity of the active compounds on cyclooxygenase isoforms was also investigated by using in vitro human "whole blood assay" and found that these derivatives did not exert their analgesic and anti-inflammatory activities through COX inhibition and other mechanisms might be involved.