Synthesis and structure-activity relationships of pyrrolidine-modified analogs of the potent cholinergic channel activator, ABT 418
1994; Elsevier BV; Volume: 4; Issue: 20 Linguagem: Inglês
10.1016/s0960-894x(01)80396-6
ISSN1464-3405
AutoresNan‐Horng Lin, Yun He, Anderson David J., James T. Wasicak, Richard Kasson, David J. Sweeny, Sullivan James P.,
Tópico(s)Cholinesterase and Neurodegenerative Diseases
Resumo3′ and 5′-substituted pyrrolidine 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. Since the primary metabolism of 1 is oxidation at the C5′ position, the effect of methyl substitution on the in vitro rate of metabolism was investigated.
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