Synthesis and structure-activity relationships of 2′-(R) and (S) pyrrolidine-modified analogs of the cholinergic channel activator, ABT-418

Abstract

2′-(R) and (S) pyrrolidine modified analogs of the potent cholinergic channel activator (ChCA), 3-methyl-5-(2(S)-pyrrolidinyl)-isoxazole (ABT-418), 1, were synthesized and tested in vitro for cholinergic channel receptor binding activity. The 4′-(S)-methyl analog of 1, the most potent compound of the 4′-substituted analogs investigated, was 6-fold less potent than 1.