Biochemical Pharmacology 1987-10-15

Dibenzoquinazoline diones as antihypertensive cyclic guanosine monophosphate phosphodiesterase inhibitors.

R F Booth, S P Buckham, D O Lunt, P W Manley, R A Porter

Index: Biochem. Pharmacol. 36(20) , 3517-21, (1987)

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Abstract

The discovery and structure-activity of a new class of renal artery phosphodiesterase inhibitors is reported, some of which are highly selective for the guanosine cyclic 3',5'-monophosphate phosphodiesterase. One of these compounds, 5,6-dihydro-8,9,11,12-tetramethoxy-1,3-dioxo-1H-benz[f]- isoquino [8,1,2- hij]quinazoline-2(3H)-carboxylic acid, ethyl ester (9), is amongst the most potent and selective compounds of this class yet identified. Furthermore, this compound demonstrates an antihypertensive effect in vivo which is presumably mediated through vascular smooth muscle relaxation.