Benzamide bioisosteres incorporating dihydroheteroazole substructures:: EPC synthesis and SAR leading to a selective dopamine D4 receptor partial agonist (FAUC 179)

被引：29

作者：

Einsiedel, J ^{[1
]}

Hübner, H ^{[1
]}

Gmeiner, P ^{[1
]}

机构：

[1] Univ Erlangen Nurnberg, Emil Fischer Ctr, Dept Med Chem, D-91052 Erlangen, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(01)00484-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Conformationally restricted benzamide bioisosteres were investigated when the chiral phenyldihydroimidazole derivative 4e (FAUC 179) showed strong and highly selective dopamine D4 receptor binding (K-ihigh=0.95nM). Mitogenesis experiments indicated partial agonist properties (42%). EPC syntheses of the target compounds of type 4 were performed starting from alpha -amino acids. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2533 / 2536

页数：4

共 34 条

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