110221-52-8

Upstream product

• 110221-43-7 (S)-2-((2S,6R)-4-Carboxymethyl-5-oxo-2-phenyl-[1,4]thiazepan-6-ylamino)-4-phenyl-butyric acid ethyl ester; hydrochloride 
• 5153-67-3 nitrostyrene 
• 1914-59-6 (E)-2-oxo-4-phenyl-3-butenoic acid 
• 110143-66-3 R-2-hydroxy-4-phenylbutyric acid L-menthyl ester 
• 29678-81-7 (R)-2-hydroxy4-phenylbutanoic acid 
• 90315-82-5 ethyl (R)-2-hydroxy-4-phenylbutyrate 
• 88767-98-0 ethyl (R)-4-phenyl-2-<<(trifluoromethyl)sulfonyl>oxy>butyrate 
• 110143-65-2 2-oxo-4-phenylbut-3-enoic acid 2-isopropyl-5-methylcyclohexyl ester 
• 110143-54-9 (2RS,6R)-6-<(tert-butoxycarbonyl)amino>-2-phenylperhydro-1,4-thiazepin-5-one 
• 111902-59-1 S-<(RS)-2-amino-1-phenylethyl>-N-(tert-butoxycarbonyl)-L-cysteine 
• 58083-14-0 N-(tert-butoxycarbonyl)-S-<(RS)-2-nitro-1-phenylethyl>-L-cysteine 
• 110221-25-5 (2S,6R)-6-amino-2-phenylperhydro-1,4-thiazepin-5-one 
• 110221-31-3 (S)-2-((2S,6R)-5-Oxo-2-phenyl-[1,4]thiazepan-6-ylamino)-4-phenyl-butyric acid ethyl ester 
• 110221-36-8 (S)-2-((2S,6R)-4-tert-Butoxycarbonylmethyl-5-oxo-2-phenyl-[1,4]thiazepan-6-ylamino)-4-phenyl-butyric acid ethyl ester 

Relevant academic research and scientific papers

Angiotensin-Converting Enzyme Inhibitors: Perhydro-1,4-thiazepin-5-one Derivatives

α-amino>-5-oxoperhydro-1,4-thiazepin-4-yl>acetic acids (monoester monoacids) and their dicarboxylic acids having the hydrophobic substituents at the 2- or 3-position of the thiazepinone ring were prepared and assayed for angiotensin-converting enzyme (ACE) inhibitory activity.The dicarboxylic acids having the pseudoequatorial amino groups at the 6-position and the pseudoequatorial hydrophobic substituents at the 2- or 3-position of the chair conformation of the thiazepinone ring had potent in vitro inhibitory activity.The monoester monoacids having the hydrophobic substituents at the 2-position suppressed pressor response to angiotensin I for a longer duration than those having the substituents at the 3-position when administered orally.The structure-activity relationship was studied by conformational energy calculations of the thiazepinone ring.

PERHYDROTHIAZEPINE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE

Compounds of formula (I): STR1 (wherein: R 1 represents an optionally substituted alkyl, cycloalkyl, aryl, partially hydrogenated aryl or heterocyclic group; R 2, R 3, R 4 and R. sup.5 represent hydrogen or an optionally substituted alkyl, cycloalkyl, aralkyl, aryl, heterocyclic or heterocyclic-alkyl group or any adjacent pair thereof form a cyclic structure, at least one not being hydrogen; A represents a bond, or a methylene, ethylene, oxymethyl or thiomethyl group; B represents an alkylene, alkylidene, cycloalkylene or cycloalkylidene group; and n is 0, 1 or 2) and salts and esters thereof are hypotensive agents.