643085-18-1Relevant academic research and scientific papers
Muscarinic subtypes profile modulation within a series of new antagonists, bridged bicyclic derivatives of 2,2-diphenyl-[1,3]-dioxolan-4-ylmethyl-dimethylamine
Piergentili, Alessandro,Gentili, Francesco,Ghelfi, Francesca,Marucci, Gabriella,Pigini, Maria,Quaglia, Wilma,Giannella, Mario
, p. 3901 - 3911 (2007/10/03)
A set of new muscarinic antagonists, bridged bicyclic derivatives of 2,2-diphenyl-[1,3]-dioxolan-4-ylmethyl-dimethylamine (1), was synthesized and tested to evaluate their affinity and selectivity for M1, M 2, M3 and M4 receptor subtypes. The conformational constraint of 1 in a bicyclic structure, and the variation in distance and stereochemistry of the active functions allowed us to modulate the selectivity of interaction with the M1-M3 receptor subtypes. The most interesting compound was (cis,trans)-2-(2,2-diphenylethyl)-5-methyl-tetrahydro-[1,3]dioxolo[4,5-c] pyrrole oxalate (6), which is equipotent with Pirenzepine on rabbit vas deferens (M1-putative) but shows a better selectivity profile.
