| Title : Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists - Gao_2002_Bioorg.Med.Chem.Lett_12_1909 |
| Author(s) : Gao LJ , Waelbroeck M , Hofman S , Van Haver D , Milanesio M , Viterbo D , De Clercq PJ |
| Ref : Bioorganic & Medicinal Chemistry Lett , 12 :1909 , 2002 |
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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 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. |
| PubMedSearch : Gao_2002_Bioorg.Med.Chem.Lett_12_1909 |
| PubMedID: 12113806 |
Gao LJ, Waelbroeck M, Hofman S, Van Haver D, Milanesio M, Viterbo D, De Clercq PJ (2002)
Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists
Bioorganic & Medicinal Chemistry Lett
12 :1909
Gao LJ, Waelbroeck M, Hofman S, Van Haver D, Milanesio M, Viterbo D, De Clercq PJ (2002)
Bioorganic & Medicinal Chemistry Lett
12 :1909