Dibenzoquinazoline diones as antihypertensive cyclic guanosine monophosphate phosphodiesterase inhibitors

Booth, R. F. G.; Buckham, S.; Lunt, David O.; Manley, Paul W.; Porter, Roderick A.

doi:10.1016/0006-2952(87)90334-0

Cited by 7 publications

(2 citation statements)

References 16 publications

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“…228 The dehydronorglaucine derivative (1 61) has been shown to be a very potent inhibitor of phosphodiesterase. 229 Treatment of dehydroglaucine with chloroform and 50% sodium hydroxide yielded (162), which was hydrolysed by hot aqueous ethanol to (163; R = CHCl,), whereas the reaction in 30% sodium hydroxide afforded the aldehyde (163; R = H). 7-Chlorodehydroglaucine, under similar conditions, gave the tetrachloro-compound (1 64).…”

Section: Benzophenanthridinesmentioning

confidence: 99%

β-Phenylethylamines and the isoquinoline alkaloids

Bentley¹

1989

Nat. Prod. Rep.

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Section: Benzophenanthridinesmentioning

confidence: 99%

β-Phenylethylamines and the isoquinoline alkaloids

Bentley¹

1989

Nat. Prod. Rep.

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“…43 Based on their mechanism of action, PDE5 inhibitors were conceived as drugs 44 and initially tested in in-vivo and ex-vivo animal models as cardiovascular, 45,46 antiplatelet, 47 antihypertensive, 48,49 and antibronchospasmatic 50 agents. The therapeutic potential of PDE5 inhibitors for the treatment of angina pectoris, congestive heart failure, myocardial infarction, hypertension, and atherosclerosis was reviewed.…”

mentioning

confidence: 99%

Phosphodiesterase 5 (PDE 5) inhibitors for the treatment of male erectile disorder: Attaining selectivity versus PDE6

Pissarnitski¹

2005

Medicinal Research Reviews

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The role of phosphodiesterase type 5 (PDE5) in the mechanism of male erection has been well understood, and several drugs inhibiting this enzyme are being used for the treatment of erectile dysfunction (ED). Discovery of inhibitors with improved selectivity versus other PDE isozymes could lead to drugs with improved safety profile. Achievement of selectivity versus PDE6, co-inhibition of which results in disturbances of color perception, remains the most challenging aspect of current drug discovery programs. The present review describes several case studies, where significant (>100 fold) selectivity versus PDE6 has been attained via investigation of structure-activity relationships (SAR). Special attention is given to the chemical routes leading to novel chemotypes and allowing efficient exploration of their SAR's. Strategies for attaining inhibitor selectivity discussed below may be applicable for other drug discovery programs.

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