- Synthesis, vasorelaxant activity and 2D-QSAR study of some novel pyridazine derivatives
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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, R2 = 0.811782, R2cvOO = 0.7153, R2cvMO = 0.7209, F = 17.9708, s2 = 9.65226 × 10-8) that was obtained employing CODESSA-Pro software.
- George, Riham F.,Saleh, Dalia O.
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p. 663 - 673
(2016/01/09)
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- Studies on the reactivity of amino-1-(6-phenyl-pyridazin-3-yl)-1H-pyrazole- 4-carboxylic acid hydrazide towards some reagents for biological evaluation
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Novel 5-amino-1-(6-phenyl-pyridazin-3-yl)-1H-pyrazole-4-carboxylic acid ethyl ester (2) was formed using (6-phenyl-pyridazin-3-yl)-hydrazine (1) and ethyl(ethoxymethylene)cyanoacetate. The β-enaminoester derivative 2 was in turn used as precursor for the
- Shamroukh, Ahmed H.,Rashad, Aymn E.,Ali, Hatem S.,Awad, Samir M.
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p. 899 - 905
(2014/08/05)
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