Historical overview, development and new approaches in design of angiotensin converting enzyme inhibitors and angiotensin receptor antagonists. Part I

Iryna Drapak; Oksana Kamenetska; Lina Perekhoda; Iryna Sych

doi:10.14748/ssp.v1i1.1506

Historical overview, development and new approaches in design of angiotensin converting enzyme inhibitors and angiotensin receptor antagonists. Part I

Iryna Drapak, Oksana Kamenetska, Lina Perekhoda, Iryna Sych

Abstract

The renin-angiotensin system (RAS) plays an important role in pathogenesis of hypertension, congestive heart failure, and chronic renal failure. In addition to a discussion of the current understanding of the chemical structures and the modes of action of angiotensin converting enzyme (ACE) inhibitors and angiotensin receptor (ATR) antagonists, review includes their SAR analysis and chemical modification for improving their activity. Nowadays different modeling strategies are underway to develop tailor made molecules with the best of properties among nonpeptide renin inhibitors, dual action receptor antagonists (e.g. angiotensin and endothelin antagonists, ACE/NEP inhibitors, AT₁/TxA₂ antagonists, balanced AT₁/AT₂ antagonists), triple inhibitors. In the first part is given an overview of various ACE inhibitors. The second part is devoted to overview of angiotensin receptor antagonists. The advances that have been made, new opportunities, and future directions of design and development of these classes have been discussed.

Keywords

renin-angiotensin system (RAS), ACE inhibitors, renin inhibitors, AT1 antagonists, AT2 antagonists, SAR analysis

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DOI: http://dx.doi.org/10.14748/ssp.v1i1.1506