Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors

被引：20
|
作者：
Novelli, F
Sparatore, A
Tasso, B
Sparatore, F
机构：
[1] Univ Genoa, Dipartimento Sci Farmaceut, I-16132 Genoa, Italy
[2] Univ Milan, Ist Chim Farmaceut & Tossicol, I-20131 Milan, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 20期
关键词：
D O I：
10.1016/S0960-894X(99)00528-4
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Quinolizidinyl derivatives of the tricyclic systems characterizing pirenzepine and nuvenzepine, were prepared and tested as ligands for muscarinic M(1), M(2) and M(3) receptors; 5,11-dihydro-11-[(S-lupinyl)-thioacetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one exhibited IC(50) = 10 nM for M(1) and 760 nM for both M2 and M3 subtypes. During the synthesis some interesting side compounds were isolated and characterized. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：3031 / 3034
页数：4
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