Synthesis, biological activity and conformational analysis of some acyclic cholinergic ligands.
A selected number of acyclic analogs of muscarine were synthesized and tested on rat jejunum. A conformational analysis carried out on compounds (I) and (II), with the Allinger's MM2 program, evidenced that their very low muscarinic activity can be related to the low percentage of the "active conformation" present in solution.
De Amici
M
M
Istituto Chimico, Farmaceutico, Università di Milano, Italy.
De Micheli
C
C
Pratesi
P
P
Toma
L
L
Grana
E
E
Santagostino-Barbone
M G
MG
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D010277:Parasympathomimetics / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
D008024:Ligands; D010277:Parasympathomimetics