DIASTEREOSELECTIVE SYNTHESIS OF MIXANPRIL, AN ORALLY-ACTIVE DUAL INHIBITOR OF NEUTRAL ENDOPEPTIDASE AND ANGIOTENSIN-CONVERTING ENZYME
DIASTEREOSELECTIVE SYNTHESIS OF MIXANPRIL, AN ORALLY-ACTIVE DUAL INHIBITOR OF NEUTRAL ENDOPEPTIDASE AND ANGIOTENSIN-CONVERTING ENZYME
复制标题
DOI：
10.1016/0960-894x(95)00316-l
复制
发表时间：
1995-09-07
影响因子：
2.7
通讯作者：
FOURNIEZALUSKI, MC
中科院分区：
文献类型：
--
作者：
TURCAUD, S;GONZALEZ, W;FOURNIEZALUSKI, MC
本文报道了一种新的非对映选择性合成mixanaline的方法，即N-[（2S，3R）-2-苯甲酰基硫甲基-3-苯基丁酰基]-L-丙氨酸，它是一种中性内肽酶和血管紧张素转换酶的双重抑制剂，可用于治疗慢性高血压和心力衰竭，为临床前筛选提供了大量的该类化合物。正如预期的那样，我们发现在麻醉大鼠中口服mixanaldehyde后，两种酶都得到了完全抑制。
A new diastereoselective synthesis of mixanpril, N-[(2S,3R)-2-benzoylthiomethyl-3-phenylbutanoyl]-L-alanine, a dual inhibitor of neutral endopeptidase and angiotensin converting enzyme, which could be used in the treatment of chronic hypertension and cardiac failure has been developed in order to obtain large quantities of this compound necessary for preclinical screening. As expected we showed that a complete inhibition of both enzymes was obtained after oral administration of mixanpril in anaesthesized rats.