Converting-enzyme inhibitors in the treatment of hypertension.

Converting-enzyme inhibitors in the treatment of hypertension.
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转化酶抑制剂治疗高血压。

DOI:
10.1056/nejm198906293202609
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发表时间:
2011
期刊:
The New England journal of medicine
影响因子:
--
通讯作者:
G. Mugesh
G. Mugesh
中科院分区:
--
文献类型:
--
作者:
B. Jyoti;G. Mugesh

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血管紧张素转换酶(ACE)催化血管紧张素I(Ang I)转化为血管紧张素II(Ang II)。血管紧张素转换酶活性与高血压有直接关系,因为血管紧张素Ⅱ是血压调节激素。因此,血管紧张素转换酶抑制剂是一类主要的抗高血压药物。卡托普利,化学名称,是1977年发现的第一种口服有效的血管紧张素转换酶抑制药物。从那时起,已经合成了许多这样的药物。酶抑制物结合的晶体结构研究揭示了对ACE活性部位抑制物相互作用的大量了解。这将有助于血管紧张素转换酶抑制剂的合理设计。随着联合治疗的进展,人们认识到具有抗氧化活性的ACE抑制剂对高血压的治疗是有益的。本研究综述了血管紧张素转换酶抑制剂在高血压治疗中的研究进展。还描述了具有抗氧化活性的ACE抑制剂的重要性。
Angiotensin converting enzyme (ACE) catalyses the conversion of angiotensin I (Ang I) to angiotensin II (Ang II). The ACE activity directly related to hypertension as Ang II is the blood pressure regulating hormone. Therefore, ACE inhibitors are a major class of antihypertensive drugs. Captopril, chemical name, was the first orally active ACE inhibitory antihypertensive drug, discovered in 1977. Since then, a number of such drugs have been synthesized. Enzyme-inhibitor bound crystal structural studies reveal a great deal of understanding about the interactions of the inhibitors at the active site of ACE. This can be helpful in the rational design of ACE inhibitors. With the advancement of the combination therapy, it is known that ACE inhibitors having antioxidant activity can be beneficial for the treatment of hypertension. This study describes the development of ACE inhibitors in the treatment of hypertension. Importance of ACE inhibitors having antioxidant activity is also described.