N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.

作者信息

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

机构信息

Discovery Chemistry and Cardiovascular Drug Discovery, Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 5400, Princeton, New Jersey 08543-5400, USA.

出版信息

J Med Chem. 2000 Apr 6;43(7):1257-63. doi: 10.1021/jm000081+.

DOI:10.1021/jm000081+

PMID:10753463

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.

摘要