Synthesis of some 3(2H)-pyridazinone and 1(2H)-phthalazinone derivatives incorporating aminothiazole moiety and investigation of their antioxidant, acetylcholinesterase, and butyrylcholinesterase inhibitory activities

Yamali C., Gulcan H. O., Kahya B., Cobanoglu S., ŞÜKÜROĞLU M. K., DOĞRUER D. S.

MEDICINAL CHEMISTRY RESEARCH, vol.24, no.3, pp.1210-1217, 2015 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 24 Issue: 3
  • Publication Date: 2015
  • Doi Number: 10.1007/s00044-014-1205-8
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.1210-1217
  • Keywords: 3(2H)-pyridazinone and 1(2H)-phthalazinone, DPPH assay, Nitric oxide assay, Cholinesterase inhibitory activity, REACTIVE OXYGEN, DISEASE, DAMAGE, MODEL, DNA
  • Gazi University Affiliated: Yes


In this study, 12 new compounds were synthesized, six of which were 3(2H)-pyridazinone (9a-f) and the others were 1(2H)-phthalazinone (10a-f) derivatives. The chemical structures of new compounds were confirmed by H-1-NMR, C-13-NMR, mass, and elemental analysis. The antioxidant properties of all the synthesized compounds were evaluated by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and nitric oxide radical scavenging assays. Moreover, cholinesterase inhibitory profiles of the synthesized compounds were determined using an in vitro assay based on a modified version of the Ellman protocol. Almost all the synthesized compounds displayed promising antioxidant activity, particularly in the DPPH radical scavenging assay, however, their inhibitory activities on cholinesterase enzymes pointed out structure specific interactions .