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Overview: Enzyme-catalyzed Enantioselective Biotransformation of Chiral Active Compounds Used in Hypertension Treatment
Current Organic Chemistry ( IF 1.7 ) Pub Date : 2020-11-30 , DOI: 10.2174/1385272824999201020204256
Joanna Chałupka 1 , Adam Sikora 1 , Aleksandra Kozicka 2 , Michał Piotr Marszałł 1
Affiliation  

Enzymatic kinetic resolution is one of the methods which allows for the synthesis of enantiomerically pure various active pharmaceutical ingredients. In contrast to chemical routes, enzymatic reactions have characteristics, including mild reaction conditions, a few byproducts, and relatively high activity of the used enzymes. β-adrenolytic drugs are widely used in the treatment of hypertension and cardiovascular disorders. Due to the fact that β- blockers possess an asymmetric carbon atom in their structure, they are presented in two enantiomeric forms. It was reported by many studies that only the (S)-enantiomers of these drugs possess the desired therapeutic effect, whereas the administration of the racemate may cause dangerous side effects, such as bronchoconstriction or diabetes. Nevertheless, β- blockers are still commercially available drugs mainly used in medicine as racemates, whereas there are several methods that are widely used in order to obtain enantiomerically pure compounds.



中文翻译:

概述:用于高血压治疗的手性活性化合物的酶催化对映选择性生物转化

酶促动力学拆分是允许合成对映体纯的各种活性药物成分的方法之一。与化学路线相反,酶促反应具有以下特征:温和的反应条件,少量副产物以及所用酶的相对较高活性。β-肾上腺皮质激素药物广泛用于治疗高血压和心血管疾病。由于β-阻滞剂在其结构中具有不对称碳原子的事实,它们以两种对映体形式存在。许多研究报告说,这些药物中只有(S)-对映异构体具有所需的治疗作用,而外消旋物的给药可能引起危险的副作用,例如支气管收缩或糖尿病。不过,

更新日期:2020-12-28
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