N-3-Substituted Imidazo Quinazolinones: Potent and Selective PDE5 Inhibitors As Potential Agents for Treatment of Erectile Dysfunction

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
John E. Macor, Bristol-Myers Squibb

Document Type

Article

Publication Date

4-6-2000

Journal / Book Title

Journal of Medicinal Chemistry

Abstract

Phosphodiesterase type 5 (PDE5) inhibitors with improved PDE isozyme selectivity relative to sildenafil may result in agents for the treatment of male erectile dysfunction (MED) with a lower incidence of PDE-associated adverse effects. This paper describes the discovery of 14, a PDE5 inhibitor with improved potency and selectivity in vitro compared to sildenafil. This compound shows activity in a functional assay of erectile function comparable to that of sildenafil.

DOI

10.1021/jm000081+

Montclair State University Digital Commons Citation

Rotella, David; Sun, Zhong; Zhu, Yeheng; Krupinski, John; Pongrac, Ronald; Seliger, Laurie; Normandin, Diane; and Macor, John E., "N-3-Substituted Imidazo Quinazolinones: Potent and Selective PDE5 Inhibitors As Potential Agents for Treatment of Erectile Dysfunction" (2000). Department of Chemistry and Biochemistry Faculty Scholarship and Creative Works. 225.
https://digitalcommons.montclair.edu/chem-biochem-facpubs/225