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Small molecule angiotensin converting enzyme inhibitors: A medicinal chemistry perspective

Affiliation
Departments of Obstetrics & Gynecology and Pediatrics ,Key Laboratory of Birth Defects and Related Diseases of Women and Children ,Ministry of Education ,West China Second University Hospital ,Sichuan University ,Chengdu ,China
Zheng, Wenyue;
Affiliation
State Key Laboratory of Oral Diseases ,National Clinical Research Center for Oral Diseases & Department of Orthodontics ,West China Hospital of Stomatology ,Sichuan University ,Chengdu ,China
Tian, Erkang;
Affiliation
State Key Laboratory of Oral Diseases ,National Clinical Research Center for Oral Diseases & Department of Orthodontics ,West China Hospital of Stomatology ,Sichuan University ,Chengdu ,China
Liu, Zhen;
Affiliation
State Key Laboratory of Oral Diseases ,National Clinical Research Center for Oral Diseases & Department of Orthodontics ,West China Hospital of Stomatology ,Sichuan University ,Chengdu ,China
Zhou, Changhan;
Affiliation
Departments of Obstetrics & Gynecology and Pediatrics ,Key Laboratory of Birth Defects and Related Diseases of Women and Children ,Ministry of Education ,West China Second University Hospital ,Sichuan University ,Chengdu ,China
Yang, Pei;
Affiliation
State Key Laboratory of Oral Diseases ,National Clinical Research Center for Oral Diseases & Department of Orthodontics ,West China Hospital of Stomatology ,Sichuan University ,Chengdu ,China
Tian, Keyue;
Affiliation
State Key Laboratory of Oral Diseases ,National Clinical Research Center for Oral Diseases & Department of Orthodontics ,West China Hospital of Stomatology ,Sichuan University ,Chengdu ,China
Liao, Wen;
Affiliation
State Key Laboratory of Oral Diseases ,National Clinical Research Center for Oral Diseases & Department of Orthodontics ,West China Hospital of Stomatology ,Sichuan University ,Chengdu ,China
Li, Juan;
Affiliation
Department of Pharmacy ,Chengdu Fifth People’s Hospital ,Chengdu ,China
Ren, Changyu

Angiotensin-converting enzyme (ACE), a zinc metalloprotein, is a central component of the renin–angiotensin system (RAS). It degrades bradykinin and other vasoactive peptides. Angiotensin-converting-enzyme inhibitors (ACE inhibitors, ACEIs) decrease the formation of angiotensin II and increase the level of bradykinin, thus relaxing blood vessels as well as reducing blood volume, lowering blood pressure and reducing oxygen consumption by the heart, which can be used to prevent and treat cardiovascular diseases and kidney diseases. Nevertheless, ACEIs are associated with a range of adverse effects such as renal insufficiency, which limits their use. In recent years, researchers have attempted to reduce the adverse effects of ACEIs by improving the selectivity of ACEIs for structural domains based on conformational relationships, and have developed a series of novel ACEIs. In this review, we have summarized the research advances of ACE inhibitors, focusing on the development sources, design strategies and analysis of structure-activity relationships and the biological activities of ACE inhibitors.

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License Holder: Copyright © 2022 Zheng, Tian, Liu, Zhou, Yang, Tian, Liao, Li and Ren.

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