Details

Autor(en) / Beteiligte

• Smith, C W
• Saneii, H H
• Sawyer, T K
• Pals, D T
• Scahill, T A
• Kamdar, B V
• Lawson, JA

Titel

Synthesis and renin inhibitory activity of angiotensinogen analogues having dehydrostatine, leu psi (CH sub(2)S)Val, or Leu psi (CH sub(2)SO)Val at the P sub(1)-P sub(1)' cleavage site

Ist Teil von

• Journal of medicinal chemistry, 1988-01, Vol.31 (7), p.1377-1382

Erscheinungsjahr

1988

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• The synthesis and in vitro renin inhibitory potencies of angiotensinogen (ANC) analogues having amide (CONH) bond replacements at P sub(1)-P sub(1)', the Leu-Val cleavage site, corresponding to Leu psi (CH sub(2)S)Val, Leu psi (CH sub(2)SO)Val, and the trans olefinic analogue of statine (Sta), 4(S)-amino-6-methyl-2(E)-heptenoci acid (dehydrostatine, Dhs), are reported. These are compared to P sub(1)-P sub(1)' Leu psi (CH sub(2)NH)Val-, Sta-, or Phe-PHe-substituted analogues of the same template. The Dhs pseudodipeptide was found to be an adequate mimic of a trans CONH bond and gave a peptide approximately equal in potency to a Phe-Phe-containing inhibitor, but 200-fold less potent than its Sta-substituted congener.