Optimization of Substituted N-3-Benzylimidazoquinazolinone Sulfonamides As Potent and Selective PDE5 Inhibitors

Authors

David Rotella, Montclair State UniversityFollow
Zhong Sun, Bristol-Myers SquibbFollow
Yeheng Zhu, Bristol-Myers SquibbFollow
John Krupinski, Bristol-Myers Squibb
Ronald Pongrac, Bristol-Myers Squibb
Laurie Seliger, Bristol-Myers SquibbFollow
Diane Normandin, Bristol-Myers SquibbFollow
J. E. Macor, Bristol-Myers Squibb

Document Type

Article

Publication Date

12-28-2000

Abstract

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.

DOI

10.1021/jm000336j

Montclair State University Digital Commons Citation

Rotella, David; Sun, Zhong; Zhu, Yeheng; Krupinski, John; Pongrac, Ronald; Seliger, Laurie; Normandin, Diane; and Macor, J. E., "Optimization of Substituted N-3-Benzylimidazoquinazolinone Sulfonamides As Potent and Selective PDE5 Inhibitors" (2000). Department of Chemistry and Biochemistry Faculty Scholarship and Creative Works. 45.
https://digitalcommons.montclair.edu/chem-biochem-facpubs/45