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ID: ALA1152170

Journal: Bioorg Med Chem Lett

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

Authors: Kim YH, Choi H, Lee J, Hwang IC, Moon SK, Kim SJ, Lee HW, Im DS, Lee SS, Ahn SK, Kim SW, Han CK, Yoon JH, Lee KJ, Choi NS.

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.

CiteXplore: 18976905

DOI: 10.1016/j.bmcl.2008.09.108