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Slow, tight binding to human renin of some nonpeptidic renin inhibitors containing a 4‐methoxymethoxypiperidinylamide at the P4 position
Author(s) -
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.
Publication year - 1992
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(92)80867-g
Subject(s) - renin–angiotensin system , position (finance) , chemistry , pharmacology , medicine , blood pressure , business , finance
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.