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

In this study, 12 new compounds were synthesized, six of which were 3(2 H )-pyridazinone ( 9a – f ) and the others were 1(2 H )-phthalazinone ( 10a–f ) derivatives. The chemical structures of new compounds were confirmed by 1 H-NMR, 13 C-NMR, mass, and elemental analysis. The antioxidant properties...

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Published inMedicinal chemistry research Vol. 24; no. 3; pp. 1210 - 1217
Main Authors Yamalı, Cem, Ozan Gülcan, H., Kahya, Burcu, Çobanoğlu, Simla, Kadir Şüküroğlu, M., Doğruer, Deniz S.
Format Journal Article
LanguageEnglish
Published Boston Springer US 01.03.2015
Subjects
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Original Research
Pharmacology/Toxicology
pyridazinone and 1
phthalazinone
Nitric oxide assay
3
Cholinesterase inhibitory activity
DPPH assay
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Summary:In this study, 12 new compounds were synthesized, six of which were 3(2 H )-pyridazinone ( 9a – f ) and the others were 1(2 H )-phthalazinone ( 10a–f ) derivatives. The chemical structures of new compounds were confirmed by 1 H-NMR, 13 C-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 .
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-014-1205-8