68709-76-2Relevant academic research and scientific papers
Angiotensin I-converting enzyme (ace) inhibitors
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Page/Page column 10, (2009/12/04)
This invention relates to a process for the synthesis of ketomethylene derivatives of the tripeptide Phe-Gly-Pro (“keto-ACE”, compound 5a) and analogues thereof. The synthesis process proceeds via an α,β-unsaturated keto intermediate. A key feature of the process involves a Horner-Emmons olefination of the, -unsaturated keto-phosphonate with ethyl glyoxylate. Keto-ACE analogues produced by the process of the invention display C-domain selectivity.
Synthesis of novel keto-ACE analogues as domain-selective angiotensin I-converting enzyme inhibitors
Nchinda, Aloysius T.,Chibale, Kelly,Redelinghuys, Pierre,Sturrock, Edward D.
, p. 4612 - 4615 (2007/10/03)
Novel analogues of the angiotensin I-converting enzyme (ACE) inhibitor keto-ACE were synthesized via a facile Horner-Emmons olefination of a phosphonoketone precursor with ethyl glyoxylate. Introduction of a bulky aromatic tryptophan at the P2
Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites
Kaltenbronn,Hudspeth,Lunney,Michniewicz,Nicolaides,Repine,Roark,Stier,Tinney,Woo,Essenburg
, p. 838 - 845 (2007/10/02)
Renin inhibitors having 13 different isosteres connecting the P3 and P2 positions have been prepared. Synthetic routes and in vitro activity exhibited by these compounds are discussed. The two most potent compounds, 47 and 48, contai
Synthesis and biological activity of ketomethylene-containing nonapeptide analogues of snake venom angiotensin converting enzyme inhibitors
Almquist,Chao,Judd,Mitoma,Rossi,Panasevich,Matthews
, p. 561 - 567 (2007/10/02)
Two ketomethylene-containing nonapeptide analogues were synthesized to determine if ketomethylene analogues of the nonapeptide venom inhibitors of angiotensin converting enzyme (ACE) would have oral ACE inhibition activity. Both ketomethylene-containing n
