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

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

Index: 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

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Citation Number: 12

Abstract

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 ...