TY - JOUR
T1 - Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists
AU - Gao, Ling Jie
AU - Waelbroeck, Magali
AU - Hofman, Sven
AU - Van Haver, Dirk
AU - Milanesio, Marco
AU - Viterbo, Davide
AU - De Clercq, Pierre J.
N1 - Funding Information:
The ‘F.W.O.’ (3G005198) and the ‘Fonds de la Recherche Scientifique Médicale’ (3.4504.99) are thanked for financial assistance. M.W. thanks Dr. N. J. Buckley (University of Leeds, UK) for the generous gift of the stably transferred CHO cells lines. Hilde Van Dingenen is thanked for some synthetic assistance.
PY - 2002/8/5
Y1 - 2002/8/5
N2 - 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.
AB - 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.
UR - https://www.scopus.com/pages/publications/0037025469
U2 - 10.1016/S0960-894X(02)00315-3
DO - 10.1016/S0960-894X(02)00315-3
M3 - Article
SN - 0960-894X
VL - 12
SP - 1909
EP - 1912
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 15
ER -