Novel and potent adenosine 3', 5'-cyclic phosphate phosphodiesterase III inhibitors: thiazolo [4, 5-b][1, 6] naphthyridin-2-ones

B Singh, ER Bacon, GY Lesher…

文献索引：Singh, Baldev; Pennock, Patrick O.; Lesher, George Y.; Bacon, Edward R.; Page, Donald F. Heterocycles, 1993 , vol. 36, # 1 p. 133 - 144

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被引用次数: 26

摘要

The transformation of 3-bromo-l, 6-naphthyridin-2 (W-ones 8 to thiazolo [4, 5-b][1, 6lnaphthyridin-2 (lH)-ones 12 resulted in a 2-9-fold increase in CAMP phosphodiesterase (PDE) I11 inhibitory potency. Unlike the secondary binding sites on the CAMP PDE I11 isozyme which interact with the methyl group of milrinone (2) and CI-930 (4), the site which interacts with the 5-substituents of 1, 6-naphthyridin-2 (WH)-ones and the 8-substituents of ...