83596-76-3Relevant academic research and scientific papers
Angiotensin converting enzyme inhibitors. (Mercaptoaroyl)amino acids
Menard,Suh,Jones,Loev,Neiss,Wilde,Schwab,Mann
, p. 328 - 332 (2007/10/02)
A series of (mercaptoaroyl)amino acids and related compounds was synthesized and tested for ability to inhibit angiotensin converting enzyme (ACE). The most active compound was N-(3-chloro-2-mercaptobenzoyl)-N-cyclo-pentylglycine, having an in vitro I50 = 0.28 μM. Substitution of the aromatic 3-position by small polar groups enhanced ACE inhibitory activity, whereas bulky groups diminished it. Alteration of the β relationship between the mercaptan and amide carbonyl or masking of the thiol by acylation reduced activity. Replacement of the thiol by nitro, hydroxy, or carboxy gave compounds lacking ACE inhibitory activity.
Aroyl-aminoacids, amides and esters thereof
-
, (2008/06/13)
Compounds of the structure STR1 wherein: Q is oxygen, sulfur or imino.X and Y are hydrogen, halogen, hydroxy, alkoxy, trifluoromethyl, nitro, carboxy, cyano, sulfonamido, sulfhydryl, alkyl, alkenyl, alkynyl, alkanoyl, alkylmercapto, amino, alkylamino, dialkylamino, alkysulfinyl, and alkylsulfonyl and may be the same or different;R 1 is hydrogen, alkanoyl, substituted alkanoyl wherein the substituent is hydroxy, amino or cycloalkyl, aroyl, arylalkanoyl, or cycloalkylcarbonyl,n is an integer from 1 to 4 inclusive,R 2 and R 3 are hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, aryl, aralkyl, and substituted derivatives thereof wherein the substituents are hydroxy, amino, alkylamino, dialkylamino, alkoxy, halogen, hydroxy, mercapto, alkylmercapto and nitro, and may be the same or different;M is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, and hetero; andZ is hydroxy, amino, alkylamino, dialkylamino, or alkoxy,have angiotensin converting enzyme inhibitory activity.
