前往化源商城

Evaluation of the side arm of (naphthylvinyl) pyridinium inhibitors of choline acetyltransferase

JF DeBernardis, P Gifford, M Rizk, R Ertel…

文献索引:DeBernardis, J. F.; Gifford, P.; Rizk, M.; Ertel, R.; Abraham, D. J.; Siuda, J. F. Journal of Medicinal Chemistry, 1988 , vol. 31, # 1 p. 117 - 121

全文:HTML全文

被引用次数: 12

摘要

A number of quaternary salts of trans-4-(/3-l-naphthylvinyl) pyridine (NVP) were synthesized and evaluated as inhibitors of the enzymes choline acetyltransferase (ChAT) and acetylcholinesterase (AChE). Structural variations in the side arm attached to the pyridine nitrogen atom demonstrate that an inductive effect is small but significant for activity. Inhibition of ChAT by alkylated derivatives decreases when electron-withdrawing groups ...