NEW HUMAN RENIN INHIBITORY PEPTIDES : ANGIOTENSINOGEN TRANSITION-STATE ANALOGUES CONTAINING NOVEL LEU-VAL REPLACEMENT AND A RETRO-INVERSO AMIDE BOND
キーワード:
bioisostere
1988 年 36 巻 6 号 p. 2278-2281
詳細
1988 年 36 巻 6 号 p. 2278-2281
New human renin inhibitors were designed from transition-state analogues of angiotensinogen, synthesized and evaluated. The peptide derovative, which contained 1-naphthylmethylsuccinylamide residue (P3) with a retro-inverso amide bond and a norstatine isoamylamide residue (P1-P1'), was stable to proteases and had potent human renin inhibitory activity. This compact inhibitor exhibited hypotension when administered orally to a monkey.
