PMID: 9181677Jan 1, 1997Paper

Synthesis and pharmacological evaluation of 4,4a,5,6-tetrahydro-7,8-disubstituted-benzo[h]cinnolin-3(2H)-ones

Il Farmaco
G A PinnaM D'Amico

Abstract

7,8-disubstituted-4,4a,5,6-tetrahydrobenzo[h]cinnolin-3(2H)-ones 2-4 have been synthesized and tested in comparison with the 8-acetylamino-4,4a,5, 6-tetrahydrobenzo[h]cinnolin-3(2H)-one 1 reported to be a potent antihypertensive and antithrombotic agent. Binding studies on phosphodiesterase (PDE) isoenzymes showed that the test compounds exhibited a modest affinity towards PDE III which in the case of 2, 3 was higher than that of 1. In vivo tests indicated that compounds 2 and 4 displayed lower hypotensive activity than model 1 while 3 was inactive. Conversely, compounds 2-4 were as potent as 1 in inhibiting collagen-induced platelet aggregation.

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