… 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…

Index: 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

Full Text: HTML

Citation Number: 49

Abstract

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. ...