Dibenzoquinazoline diones as antihypertensive cyclic guanosine monophosphate phosphodiesterase inhibitors

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]-...

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Bibliographic Details
Published inBiochemical pharmacology Vol. 36; no. 20; p. 3517
Main Authors Booth, R F, Buckham, S P, Lunt, D O, Manley, P W, Porter, R A
Format Journal Article
LanguageEnglish
Published England 15.10.1987
Subjects
3',5'-Cyclic-GMP Phosphodiesterases - antagonists & inhibitors
Animals
Antihypertensive Agents - pharmacology
Cattle
Isoquinolines - pharmacology
Rats
Rats, Inbred SHR
Structure-Activity Relationship
Tetrahydroisoquinolines
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Summary: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.
ISSN:0006-2952
DOI:10.1016/0006-2952(87)90334-0