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

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

文献索引: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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被引用次数: 24

摘要

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 ...