首次通过酶促水解/硫迈克尔加成级联反应路线合成 AChE 抑制剂。
First enzymatic hydrolysis/thio-Michael addition cascade route to synthesis of AChE inhibitors.
机构信息
Normandie Univ, COBRA, UMR 6014 & FR 3038; Univ Rouen; INSA Rouen; CNRS, 1 rue Tesnière 76821 Mont-Saint-Aignan, Cedex, France.
出版信息
Chem Commun (Camb). 2014 Feb 25;50(16):2043-5. doi: 10.1039/c3cc48871c.
PMID:24418813
Abstract
The irreversible Michael addition of thiols to acrylamides is reported as a new tool for the kinetic target-guided synthesis. In an unprecedented enzymatic hydrolysis/thio-Michael addition procedure, potent and selective acetylcholinesterase inhibitors are assembled by the enzyme using both its esterasic and templating ability.
摘要
据报道，巯基与丙烯酰胺的不可逆迈克尔加成是一种新的动力学靶向合成工具。在一种前所未有的酶促水解/硫迈克尔加成过程中，酶利用其酯酶和模板能力来组装有效的和选择性的乙酰胆碱酯酶抑制剂。
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