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Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists

Authors :
Gao, Ling-Jie
Waelbroeck, Magali
Hofman, Sven
Van Haver, Dirk
Milanesio, Marco
Viterbo, Davide
De Clercq, Pierre J.
Source :
Bioorganic & Medicinal Chemistry Letters. Aug2002, Vol. 12 Issue 15, p1909. 4p.
Publication Year :
2002

Abstract

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 M1–M4 muscarine receptor subtypes revealed that analogues 3a and 5c display a promising 10-fold selectivity for the M2 receptor as compared to the M1 receptor. [Copyright &y& Elsevier]

Subjects

Subjects :
*UNSATURATED compounds
*CARBON

Details

Language :
English
ISSN :
0960894X
Volume :
12
Issue :
15
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
7837537
Full Text :
https://doi.org/10.1016/S0960-894X(02)00315-3