| Literature DB >> 17084634 |
Alessandro Piergentili1, Wilma Quaglia, Mario Giannella, Fabio Del Bello, Bruno Bruni, Michela Buccioni, Antonio Carrieri, Samuele Ciattini.
Abstract
Muscarinic agonists, bearing 1,4-dioxane and 1,4-oxathiane nuclei, were synthesized and tested to evaluate their potency at M(1)-M(4) muscarinic receptor subtypes. The stereochemical relationship between the 2-side chain and the 6-methyl group plays an important role in drug-receptor interaction, since the cis isomers are more potent than the corresponding trans isomers. However, the latter are able to discriminate between the muscarinic receptor subtypes. Among them compound 5b proves particularly interesting, since it selectively activates the ileal M(3) receptor subtype and is devoid of agonist activity at the others.Entities:
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Year: 2006 PMID： 17084634 DOI： 10.1016/j.bmc.2006.10.040
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641