Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists

被引：14

作者：

Gao, LJ

Waelbroeck, M

Hofman, S

Van Haver, D

Milanesio, M

Viterbo, D

De Clercq, PJ

机构：

[1] Univ Ghent, Dept Organ Chem, B-9000 Ghent, Belgium

[2] Univ Piemonte Orientale, Dipartimento Sci & Tecnol Avanzate, I-15100 Alessandria, Italy

[3] Free Univ Brussels, Lab Chim Biol & Nutr, B-1070 Brussels, Belgium

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(02)00315-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of himbacine (1)-related analogues has been prepared featuring three different isomeric configurations with respect to the B-ring (a, b and natural c) and three different interconnecting two-carbon unsaturated units [natural (E)-ene, (Z)-ene, and yne]. The study of the binding affinities of the nine resulting compounds, including synthetic (+)-himbacine (3c), towards the M-1-M-4 muscarine receptor subtypes revealed that analogues 3a and 5c display a promising 10-fold selectivity for the M-2 receptor as compared to the M, receptor. (C) 2002 Elsevier Science Ltd. All rights reserved.

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页码：1909 / 1912

页数：4

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