Synthesis, vasorelaxant activity and 2D-QSAR study of some novel pyridazine derivatives.

Synthesis, vasorelaxant activity and 2D-QSAR study of some novel pyridazine derivatives.
Eur J Med Chem. 2015 Dec 12;108:663-673
Authors: George RF, Saleh DO
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.
PMID: 26735908 [PubMed - as supplied by publisher]

Source: European Journal of Medicinal Chemistry - December 12, 2015 Category: Chemistry Authors: George RF, Saleh DO Tags: Eur J Med Chem Source Type: research