Heteroaromatic and aniline derivatives of piperidines as potent ligands for vesicular acetylcholine transporter

…, D Zeng, NP Rath, H Flores, JS Perlmutter…

Index: Li, Junfeng; Zhang, Xiang; Zhang, Zhanbin; Padakanti, Prashanth K.; Jin, Hongjun; Cui, Jinquan; Li, Aixiao; Zeng, Dexing; Rath, Nigam P.; Flores, Hubert; Perlmutter, Joel S.; Parsons, Stanley M.; Tu, Zhude Journal of Medicinal Chemistry, 2013 , vol. 56, # 15 p. 6216 - 6233

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Citation Number: 12

Abstract

To identify suitable lipophilic compounds having high potency and selectivity for vesicular acetylcholine transporter (VAChT), a heteroaromatic ring or a phenyl group was introduced into the carbonyl-containing scaffold for VAChT ligands. Twenty new compounds with ALogD values between 0.53 and 3.2 were synthesized, and their in vitro binding affinities were assayed. Six of them (19a, 19e, 19g, 19k, and 24a–b) displayed high affinity for ...