… activity of 6-carbethoxy-and 6-ethoxy-3, 7-disubstituted pyrazolo [1, 5-a] pyrimidines and related derivatives as adenosine cyclic 3', 5'-phosphate phosphodiesterase …

…, MB Scholten, DE O'Brien, T Novinson…

文献索引：Springer, Robert H.; Scholten, M. B.; O'Brien, Darrell E.; Novinson, Thomas; Miller, Jon P.; Robins, Roland K. Journal of Medicinal Chemistry, 1982 , vol. 25, # 3 p. 235 - 242

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被引用次数: 49

摘要

A number of 3,7-disubstituted 6-carbethoxypyrazolo[ 1,5-a]pyrimidines and 3,7-disubstituted 6-ethoxypyrazolo- [ 1,5-a]pyrimidines have been prepared and evaluated as adenosine cyclic 3',5'-phosphate (CAMP) phosphodiesterase (PDE) inhibitors vs. the low K, enzyme isolated from beef heart, rabbit lung, and kidney preparations. The results were found to be between 0.5 to 13 times as potent as theophylline as inhibitors of PDE, depending on the tissue source. ...