Literature DB >> 24997281

How to design a potent, specific, and stable angiotensin-converting enzyme inhibitor.

Katarzyna Regulska1, Beata Stanisz2, Miłosz Regulski3, Marek Murias3.   

Abstract

Angiotensin-converting enzyme inhibitors (ACE-Is) are a valuable class of antihypertensive drugs used in the treatment of cardiovascular system-related diseases. Hence, constant research into, and the development of, such compounds remain within the priorities of modern medical sciences. In this respect, a thorough understanding of their chemistry and biology is an important aspect of drug design; therefore, we present here available data on the pharmaceutical properties of ACE-Is. We also review the structural and biochemical features of the molecular target of ACE-Is and demonstrate several known enzyme-inhibitor complexes. Finally, we attempt to create a mathematical model describing the relation between the potency and/or stability of ACE-Is and their structural characteristics using quantitative structure-activity relation (QSAR), and quantitative structure-property relation (QSPR) techniques.
Copyright © 2014 Elsevier Ltd. All rights reserved.

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Year:  2014        PMID: 24997281     DOI: 10.1016/j.drudis.2014.06.026

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN: 1359-6446            Impact factor:   7.851


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  5 in total

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