68074-17-9

Upstream product

• 68074-14-6 3-methylidene-2-oxo-piperidine 
• 25474-85-5 4-methoxybenzyloxycarbonyl azide 
• 68074-16-8 2-Methylene-5-(p-methoxybenzyloxycarbonyl)aminopentanoic acid 

Relevant academic research and scientific papers

ORALLY EFFECTIVE ANTI-HYPERTENSIVE AGENTS

Novel thiolester compounds are disclosed which are orally effective angiotensin converting enzyme inhibitors useful in the treatment of mammalian hypertension. They have the formula, EQU1 wherein Z denotes-B-A 2, R 1 is H or an acyl group, A 1 is a carboxylic acid containing at least one amino or imino-N-, A 2 is a carboxylic acid containing at least one amino or imino-N-or a lower alkyl ester or amide thereof, B is a 2-4 carbon backbone chain in mercapto linkage to S which includes a carbonyl or sulfonyl group joined in carboxamido or sulfonamido linkage, respectively, to A 2. Preferably A 2 includes a 4-6 membered C-N ring or a 5 membered ring of one N, one S and 3 C atoms.

Anti-hypertensive agents

Novel inhibitors of angiotensin converting enzyme having the general formula R--A--S--Z are disclosed as potent inhibitors of angiotensin converting enzyme and are useful anti-hypertensive agents.

Amino acid derivatives

A method for alleviating or reducing angiotensin related hypertension in hypertensive mammals comprises administering an effective amount of a compound having the general formula STR1 Intermediates for the preparation of such compounds are also included.

AMINO ACID DERIVATIVES

New substituted acyl derivatives of amino acids which have the general formula STR1 are useful as angiotensin converting enzyme inhibitors.

Design of potent and specific inhibitors of carboxypeptidases A and B.

The combination in one molecule of functional groups that can interact specifically with different substrate binding areas at the active site of carboxypeptidases A and B has led to the development of potent and specific inhibitors of these enzymes. 2-Benzyl-3-mercaptopropanoic acid (SQ 14,603) has a Ki of 1.1 x 10(-8) M vs. carboxypeptidase A and a Ki of 1.6 x 10(-4) M vs. the B enzyme. 2-Mercaptomethyl-5-guanidinopentanoic acid (SQ 24,798) has a Ki of 4 x 10(-10) M vs. carboxypeptidase B and a Ki of 1.2 x 10(-5) M vs. carboxypeptidase A. It is proposed that the sulfhydryl groups of these inhibitors bind to the catalytically important zinc ions of these enzymes, and that, in conjunction with the benzyl and guanidinopropyl side chains, they are responsible for their specificity.