新型褪黑素-他克林杂合二聚体对丁酰胆碱酯酶的高选择性抑制。
Highly selective inhibition of butyrylcholinesterase by a novel melatonin-tacrine heterodimers.
机构信息
Faculty of Chemistry, University of Warsaw, Warsaw, Poland.
出版信息
J Pineal Res. 2013 May;54(4):435-41. doi: 10.1111/jpi.12006.
Novel inhibitors of cholinesterases, especially butyrylcholinesterase (BuChE), were obtained by coupling melatonin-tacrine heterodimers via the carbamate bond. Compounds 14a-i possessed potent cholinesterase inhibitory activity (with IC50 values as low as 1.18 nM for acetylcholinesterase (AChE) and 0.24 nM for butyrylcholinesterase (BuChE)). These heterodimers exhibit selectivity toward BuChE, being from 4- to 256-fold more active toward BuChE than AChE, but still acting as better AChE inhibitors than tacrine 4.
通过氨基甲酸酯键将褪黑素-他克林杂合二聚体偶联，获得了新型的胆碱酯酶抑制剂，特别是丁酰胆碱酯酶（BuChE）抑制剂。化合物 14a-i 对乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BuChE）具有很强的抑制活性（IC50 值分别低至 1.18 nM 和 0.24 nM）。这些杂合二聚体对 BuChE 具有选择性，对 BuChE 的活性比 AChE 高 4-256 倍，但仍比他克林 4 对 AChE 的抑制作用更强。
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