B. Pieper et al., LACTONES .28. EPC-SYNTHESIS, STRUCTURE AN D PHARMACOLOGY OF LACTONIZED AND LACTAMIZED ANALOGS OF ACETYLCHOLINE, Die Pharmazie, 50(1), 1995, pp. 15-21
The enantiopure gamma-aminomethyl-gamma-butyrolactones (S)- and (R)-4a
-d represent constrained analogues of acetylcholine, which were synthe
sized from D- or L-glutamic acid following two different routes. In ad
dition, the corresponding lactames (S)- and (R)-10 were prepared by en
antioselective synthesis. Only moderate activity was found at acetylch
oline sites at the guinea pig atrium.