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Updated: Mar 27, 2026

Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Synthesis, vasorelaxant activity and 2D-QSAR study of some novel pyridazine derivatives
Riham F George1, Dalia O Saleh2
1Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, ElKasr El-Aini Street, 11562 Cairo, Egypt.
Abstract:
Novel 3,6-disubstituted pyridazines were synthesized by facile method and screened for their vasorelaxant properties utilizing isolated thoracic rat aortic rings. Compounds 8a and 11a exerted potent vasorelaxant activity (IC50 = 198 and 177 μM, respectively) relative to doxazosin mesylate (used reference standard, IC50 = 226 μM), that, they may represent promising hits for treatment of cardiovascular disorders. The observed activity was validated by a statistically significant QSAR model (N = 32, n = 6, R(2) = 0.811782, R(2)cvOO = 0.7153, R(2)cvMO = 0.7209, F = 17.9708, s(2) = 9.65226 × 10(-8)) that was obtained employing CODESSA-Pro software.
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