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.
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页码：3031 / 3034
页数：4
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