131124-75-9Relevant academic research and scientific papers
Synthesis and biological activity of N-terminus modified angiotensin II analogues
Bovy, P. R.,O'Neal, J. M.,McMahon, E.,Palomo, M.,Smits, G. J.,et al.
, p. 589 - 594 (2007/10/02)
Semi-peptidic analogues of the angiotensin II (AII) antagonist AII have been prepared by the solid phase method and, for some steps, by synthesis in solution.In the modified analogues 4-15, the N-terminal di- or tripeptidic fragments (Asp-Arg or Asp-Arg-Val) in AII was replaced by non-peptidic moieties featuring amino or guanidino groups as substituent of simple alkyl spacers of various lengths.The compounds synthesized have been tested for their ability to produce an AII-like contraction and/or to inhibit AII-induced contractions in isolated rabbit aortae.All of them were found devoid of agonistic activity and most retained significant antagonistic activity in this assay.Analogue 5 antagonized AII-induced blood pressure effect in the anesthetized rat when infused at 30 μg/kg/min.The structure-activity relationships for these compounds are discussed.
