PDE5 inhibitors: an original access to novel potent arylated analogues of tadalafil

T Beghyn, C Hounsou, BP Deprez

Index: Beghyn, Terence; Hounsou, Candide; Deprez, Benoit P. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 3 p. 789 - 792

Full Text: HTML

Citation Number: 20

Abstract

A method to access totally new analogues of tadalafil was explored. The Buchwald reaction was adapted and used to replace the methyl group of tadalafil by various aryl groups. Inhibition potencies on PDE5 of these analogues were determined and proved to be comparable to the one of tadalafil. Using the same route, compounds with the same level of activity but improved water solubility were produced by introducing a pyridine or a ...