Furoyl and Benzofuroyl Pyrroloquinolones as Potent and Selective PDE5 Inhibitors for Treatment of Erectile Dysfunction

Journal of Medicinal Chemistry
2003.0

Abstract

Synthesis of furoyl and benzofuroyl pyrroloquinolones as potent and selective PDE5 inhibitors was reported. Their in vitro potencies in inhibiting PDE5 and selectivity in inhibiting other PDE isozymes (PDE1-4 and PDE6) were evaluated. Some of these compounds are more potent than sildenafil with better selectivity toward PDE1 and PDE6. Incorporation of solublizing groups resulted in bioavailable analogues. Selected compounds showed in vivo efficacy in anesthetized dog model for penile erection.

Knowledge Graph

Similar Paper

Furoyl and Benzofuroyl Pyrroloquinolones as Potent and Selective PDE5 Inhibitors for Treatment of Erectile Dysfunction
Journal of Medicinal Chemistry 2003.0
Pyrimidinylpyrroloquinolones as Highly Potent and Selective PDE5 Inhibitors for Treatment of Erectile Dysfunction
Journal of Medicinal Chemistry 2002.0
Substituted Pyrazolopyridopyridazines as Orally Bioavailable Potent and Selective PDE5 Inhibitors:  Potential Agents for Treatment of Erectile Dysfunction
Journal of Medicinal Chemistry 2003.0
Structure−Activity Relationships of N-Acyl Pyrroloquinolone PDE-5 Inhibitors
Journal of Medicinal Chemistry 2004.0
Pyrroloquinolone PDE5 Inhibitors with Improved Pharmaceutical Profiles for Clinical Studies on Erectile Dysfunction
Journal of Medicinal Chemistry 2005.0
Quinazolines as potent and highly selective PDE5 inhibitors as potential therapeutics for male erectile dysfunction
Bioorganic & Medicinal Chemistry Letters 2008.0
Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction
Bioorganic & Medicinal Chemistry Letters 2004.0
Substituted Pyrazolopyridines as Potent and Selective PDE5 Inhibitors:  Potential Agents for Treatment of Erectile Dysfunction
Journal of Medicinal Chemistry 2001.0
Synthesis and biological activities of novel β-Carbolines as PDE5 inhibitors
Bioorganic & Medicinal Chemistry Letters 2003.0
2-Phenylquinazolin-4(3H)-one, a class of potent PDE5 inhibitors with high selectivity versus PDE6
Bioorganic & Medicinal Chemistry Letters 2009.0