| Literature DB >> 26735908 |
Riham F George1, Dalia O Saleh2.
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.Entities:
Keywords: Pyridazines; QSAR; Vasodilator
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Year: 2015 PMID： 26735908 DOI： 10.1016/j.ejmech.2015.12.015
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514