1, 4-Bis (3-oxo-2, 3-dihydropyridazin-6-yl) benzene analogs: potent phosphodiesterase inhibitors and inodilators

…, HD Prain, ML Reeves, BH Warrington

文献索引：Coates, William J.; Prain, H. Douglas; Reeves, Martin L.; Warrington, Brian H. Journal of Medicinal Chemistry, 1990 ,  vol. 33,  # 6  p. 1735 - 1741

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被引用次数: 30

摘要

These novel compounds were evaluated for inhibition of the low K,, CAMP-selective, cGMP- inhibited phosphodiesterase (PDE 111) derived from cat heart and hemodynamic activity in the ganglion-and@-blocked anesthetized cat. The most potent PDE I11 inhibitor of the series was 6-[4-(5-methyl-3-0~ 0-2, 3, 4, 5-tetrahydropyridazin-6-y1)-phenyl] pyridazin-3 (2H)-one (ICm= 0.07 pM), which also retained the greatest inotrope and vasodilator ( ...