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

被引：27
作者：
Beghyn, Terence
Hounsou, Candide
Deprez, Benoit P.
机构：
[1] Inserm U761, F-59006 Lille, France
[2] Univ Lille 2, Fac Pharm, Inst Pasteur Lille, Lille, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 03期
关键词：
PDE5; tadalafil; tetrahydrobetacarboline; N-arylation; cuprous iodide; epimerisation;
D O I：
10.1016/j.bmcl.2006.10.069
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
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 tadalafit 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. (c) 2006 Elsevier Ltd. All rights reserved.
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收藏
页码：789 / 792
页数：4
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