Slow, tight binding to human renin of some nonpeptidic renin inhibitors containing a 4‐methoxymethoxypiperidinylamide at the P4 position

Autor: Stein, Herman H., Fung, Anthony K.L., Cohen, Jerome, Baker, William R., Rosenberg, Saul H., Boyd, Steven A., Dayton, Brian D., Armiger, Yoek Lin S.-T., Condon, Stephen L., Mantei, Robert A., Kleinert, Hollis D.
Zdroj: FEBS Letters; April 1992, Vol. 300 Issue: 3 p301-304, 4p
Abstrakt: A series of nonpeptidic human renin inhibitors with a 4‐methoxymethoxypiperidinylamide at the P4 position of the molecule exhibited slow tight binding to the enzyme. Replacement of the methoxymethoxy moiety on the piperidine ring with H, OH, methoxyethyl, propyloxy or n‐butyl eliminated the effect. The inhibition was partially reversed by prolonged dialysis at 4°C, arguing against formation of a covalent bond in the tightened complex.
Databáze: Supplemental Index