Differential binding of phenothiazine urea derivatives to wild-type human cholinesterases and butyrylcholinesterase mutants

…, KV Darvesh, RS McDonald, R Walsh, S Conrad…

Index: Darvesh, Sultan; Pottie, Ian R.; Darvesh, Katherine V.; McDonald, Robert S.; Walsh, Ryan; Conrad, Sarah; Penwell, Andrea; Mataija, Diane; Martin, Earl Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 6 p. 2232 - 2244

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Citation Number: 24

Abstract

A series of N-10 urea derivatives of phenothiazine was synthesized and each compound was evaluated for its ability to inhibit human cholinesterases. Most were specific inhibitors of BuChE. However, the potent inhibitory effects on both cholinesterases of one sub-class, the cationic aminoureas, provide an additional binding mechanism to cholinesterases for these compounds. The comparative effects of aminoureas on wild-type BuChE and several ...