Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction

…, J Krupinski, D Normandin, R Pongrac, L Seliger…

Index: Bi, Yingzhi; Stoy, Patrick; Adam, Leonard; He, Bin; Krupinski, John; Normandin, Diane; Pongrac, Ron; Seliger, Laurie; Watson, Andrew; Macor, John E. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 6 p. 1577 - 1580

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Citation Number: 29

Abstract

In a continuing effort to discover novel chemotypes as potent and selective PDE5 inhibitors for the treatment of male erectile dysfunction (ED), we have found that 4- benzylaminoquinoline derivatives are very potent and selective PDE5 inhibitors. Some compounds in this series had PDE5 IC50's as low as 50 pM. While an electron withdrawing group at the C6-position of the quinoline substantially improved PDE5 potency, an ethyl ...