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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Cage amines as the stopper inhibitors of cholinesterases.
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Cage amines as the stopper inhibitors of cholinesterases.

机译:笼型胺作为胆碱酯酶的终止剂。

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摘要

Cage amines 1-4 are potent peripheral anionic site-bound reversible inhibitors of both acetylcholinesterase and butyrylcholinesterase. Cage amines 1-3 are selective butyrylcholinesterase inhibitor versus acetylcholinesterase. For both enzymes, the -log K(i) values linearly correlate with the difference of substituted phenyl radius of cage amines (-log K(i)=5.4+3.4Deltagamma for acetylcholinesterase, -log K(i)=5.9+3.2Deltagamma for butyrylcholinesterase). Moreover, the relationship between the enzymes and cage amines mimics that between bottles and stoppers.
机译:笼型胺1-4是乙酰胆碱酯酶和丁酰胆碱酯酶的有效的外围阴离子位点结合的可逆抑制剂。笼胺1-3是选择性丁酰胆碱酯酶抑制剂,而不是乙酰胆碱酯酶。对于这两种酶,-log K(i)值均与笼型胺的取代苯基半径之差线性相关(对于乙酰胆碱酯酶,-log K(i)= 5.4 + 3.4Deltagamma,-log K(i)= 5.9 + 3.2Deltagamma用于丁酰胆碱酯酶)。此外,酶和笼型胺之间的关系类似于瓶子和塞子之间的关系。

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