Assessing biocatalysis for the synthesis of optically active tetrahydropyrazolo[1,5-α]pyrimidines (THPPs) as novel therapeutic agents
Assessing biocatalysis for the synthesis of optically active tetrahydropyrazolo[1,5-α]pyrimidines (THPPs) as novel therapeutic agents
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DOI：
10.1016/j.molcatb.2013.11.012
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发表时间：
2014-02-01
影响因子：
--
通讯作者：
Remuinan-Blanco, Modesto J.
中科院分区：
文献类型：
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作者：
Fernandez-Alvaro, Elena;Esquivias, Jorge;Remuinan-Blanco, Modesto J.
对映体纯的THPP在结核病、骨质疏松症和丙型肝炎等相关治疗领域是有用的药理学试剂。通常通过制备型手性HPLC解析，在这项工作中，催化方法-通过水解酶催化的动力学拆分-已首次得到证实。在生物催化成功的概念验证之后，蛋白质工程和工艺设置的未来机会出现了。(C)2013爱思唯尔有限公司版权所有。
Enantiomerically pure THPPs are useful pharmacological agents in relevant therapeutic areas such as tuberculosis, osteoporosis and hepatitis C. Typically resolved by preparative chiral HPLC, in this work the catalytic approach - via hydrolase-catalyzed kinetic resolution - has been demonstrated for the first time. After biocatalytic successful proof-of-concept, future opportunities for protein engineering and process set-up appear. (C) 2013 Elsevier B.V. All rights reserved.