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

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• 作者：Terence Beghyn ; C ; ide Hounsou ; Benoit P. Deprez
• 关键词：PDE5 ; Tadalafil ; Tetrahydrobetacarboline ; N-arylation ; Cuprous iodide ; Epimerisation
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 February 2007
• 卷：17
• 期：3
• 页码：789-792
• 文件大小：150 K

摘要

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 pyrimidine ring. This original route also opens access to new unpatented compounds.