Optimization of substituted N-3-benzylimidazoquinazolinone sulfonamides as potent and selective PDE5 inhibitors

D. P. Rotella, Z. Sun, Y. Zhu, J. Krupinski, R. Pongrac, L. Seliger, D. Normandin, J. E. Macor

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A previous report from these laboratories identified the N-3-benzylimidazoquinazolinone nucleus as a more selective PDE5 inhibitor template compared to the pyrazolopyrimidine of sildenafil. This paper describes in detail the structure-activity relationships of a set of sulfonamide analogues, several of which are both more potent and more selective PDE5 inhibitors in vitro than sildenafil. The synthesis, in vitro enzyme activity and selectivity, and in vitro functional and preclinical pharmacokinetic assessment of molecules in this series are described.

Original languageEnglish
Pages (from-to)5037-5043
Number of pages7
JournalJournal of Medicinal Chemistry
Issue number26
StatePublished - 28 Dec 2000


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