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Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists.

par Gao, Ling-Jie;Waelbroeck, Magali ;Hofman, Sven;Van Haver, Dirk;Milanesio, Marco;Viterbo, Davide;De Clercq, Pierre
Référence Bioorganic & medicinal chemistry letters, 12, 15, page (1909-1912)
Publication Publié, 2002-08

Article révisé par les pairs

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Résumé :

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(1) receptor.