95272-47-2Relevant academic research and scientific papers
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.
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.
Pharmaceutical amides, and preparation, formulations and use of thereof
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, (2008/06/13)
Compounds of the general formula STR1 wherein Ph is a phenyl group which is optionally substituted by one or more substituents selected from halo (i.e. fluoro, chloro, bromo or iodo), C1-4 alkyl, amino, C1-4 alkylamino, di-C1-4 alkylamino, nitro, sulphonyl, aminosulphonyl, trihalomethyl, carboxy, C1-4 alkoxycarbonyl, amido, C1-4 alkylamido C1-4 alkoxy, C2-4 alkenyl, cyano, aminomethyl or methylsulphonyl; Ra and Rb, which may be the same or different, each represents a hydrogen or alkali metal (e.g. sodium or lithium) atom or a C1-4 (e.g. ethyl) group; m is 0 or 1; Y is a group of formula: or a group of formula: STR2 where R1 is hydrogen or methyl; R2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is --OR3 or --NR4 R5 where R3, R4 and R5 are each hydrogen or alkyl of 1 to 4 carbon atoms (i.e. methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, or t-butyl) and R3 can further be phenylalkyl having 1 to 3 carbon atoms in the alkylene moiety thereof, or phenyl; and basic salts thereof. These compounds have an advantageous enkephalinase inhibitory activity which renders the compounds useful in medical therapy, e.g. to prolong and/or potentiate in a mammal, the effects of endogenous or exogenous enkephalins. The latter includes synthetic enkepalin analogues.
