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

被引：30

作者：

Kim, Young Hoon ^{[1
,4
]}

Choi, Hojin ^{[1
]}

Lee, Jaekwang ^{[1
]}

Hwang, In-Chang ^{[1
]}

Moon, Seung Kee ^{[1
]}

Kim, Soo Jin ^{[1
]}

Lee, Hong Woo ^{[1
]}

Im, Dai Sig ^{[1
]}

Lee, Sung Sook ^{[1
]}

Ahn, Soon Kil ^{[1
]}

Kim, Sang Woong ^{[2
]}

Han, Cheol Kyu ^{[3
]}

Yoon, Jeong Hyeok ^{[3
]}

Lee, Kyung Joo ^{[1
]}

Choi, Nam Song ^{[1
]}

机构：

[1] CKD Pharmaceut Inc, Chong Kun Dang Res Inst, Cheonan, South Korea

[2] LeadGenex, Venture Town Dasan, Taejon, South Korea

[3] Equispharm Inc, Gyeonggi Bioctr, Suwon 443766, Gyeonggi Do, South Korea

[4] Soong Sil Univ, Dept Chem, Seoul 156743, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 23期

关键词：

PDE5; PDE6; PDE11; Inhibitor; Quinazoline; MED;

D O I：

10.1016/j.bmcl.2008.09.108

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6279 / 6282

页数：4

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