3-Thio-quinolinone maxi-K openers for the treatment of erectile dysfunction.

作者信息

Boy Kenneth M, Guernon Jason M, Sit Sing-Yuen, Xie Kai, Hewawasam Piyasena, Boissard Christopher G, Dworetzky Steven I, Natale Joanne, Gribkoff Valentin K, Lodge Nicholas, Starrett John E

机构信息

Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA.

出版信息

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5089-93. doi: 10.1016/j.bmcl.2004.07.080.

A series of Maxi-K openers for the treatment of erectile dysfunction based on the 3-thio-quinolinone core is described. Significant levels of channel opening (up to 550% of control) are seen in transfected oocytes. Functional activity in rabbit corpus cavernosum tissue strips confirms the potential to effect therapy for ED, the effect being maximal for the 3-amino-2-hydroxy thiol side chain.