105852-84-4Relevant academic research and scientific papers
NOVEL 5-AMINO-4-HYDROXYVALERYL DERIVATIVES
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, (2008/06/13)
Compounds of the formula STR1 in which R 1 represents hydrogen or acyl, A represents an optionally N-alkylated α-amino acid residue which is bonded N-terminally to R 1 and C-terminally to the group--NR 2--, R 2 represents hydrogen or lower alkyl, R 3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R 4 represents hydroxy or etherified or esterified hydroxy, R 5 represents lower alkyl having 2 or more carbon atoms, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy or optionally substituted mercapto and R 6 represents substituted amino, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as antihypertensives.
Synthesis and biological activity of some transition-state inhibitors of human renin
Buhlmayer,Caselli,Fuhrer,Goschke,Rasetti,Rueger,Stanton,Criscione,Wood
, p. 1839 - 1846 (2007/10/02)
A series of renin inhibitors containing the dipeptide transition state mimics (2S,4S,5S)-5-amino-4-hydroxy-2-isopropyl-7-methyloctanoic acid (Leu-(OH)-Val) and (2S,4S,5S)-5-amino-4-hydroxy-2-isopropyl-6-cyclohexylhexanoic acid (Cha-(OH)-Val) was prepared.
