Quinazolines as potent and highly selective PDE5 inhibitors as potential therapeutics for male erectile dysfunction.

Abstract

In an effort to minimize side effects associated with low selectivity against PDE isozymes, we have successfully identified a series of 6,7,8-substituted quinzaolines as potent inhibitors of PDE5 with high level of isozyme selectivity, especially against PDE6 and PDE11. PDE5 potency and isozyme selectivity of quinazolines were greatly improved with substitutions both at 6- and 8-position. The synthesis, structure-activity relationships and in vivo efficacy of this novel series of potent PDE5 inhibitors are described.

• Authors: Young Hoon Kim, Hojin Choi, Jaekwang Lee, In-Chang Hwang, Seung Kee Moon, Soo Jin Kim, Hong Woo Lee, Dai Sig Im, Sung Sook Lee, Soon Kil Ahn, Sang Woong Kim, Cheol Kyu Han, Jeong Hyeok Yoon, Kyung Joo Lee, Nam Song Choi
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 18 Issue 23 Pg. 6279-82 (Dec 01 2008) ISSN: 1464-3405 [Electronic] England
• PMID: 18976905 (Publication Type: Journal Article)

Chemical References

• Phosphodiesterase 5 Inhibitors
• Phosphodiesterase Inhibitors
• Quinazolines

Topics

• Combinatorial Chemistry Techniques
• Erectile Dysfunction (drug therapy)
• Humans
• Male
• Molecular Structure
• Penile Erection (drug effects)
• Phosphodiesterase 5 Inhibitors
• Phosphodiesterase Inhibitors (chemical synthesis, therapeutic use)
• Quinazolines (chemical synthesis, therapeutic use)
• Structure-Activity Relationship