25528-71-6Relevant articles and documents
DIAMINOPROPANOL RENIN INHIBITORS
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Page/Page column 90-91, (2008/06/13)
Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of renin activity or in the treatment of aspartic protease me
Conjugate additions of organocuprates to a 3-methylene-6-isopropyldiketopiperazine acceptor for the asymmetric synthesis of homochiral α-amino acids
Bull,Davies,Garner,O'Shea
, p. 3281 - 3287 (2007/10/03)
Addition of a range of organocuprates to (S)-N,N′-bis(p-methoxybenzyl)-3-methylene-6-isopropylpiperazine-2, 5-dione 8 affords cis-3-isopropyl-6-alkyldiketopiperazines in excellent yield and >95% de. Subsequent deprotection and hydrolysis of these cis-3-isopropyl-6-alkyldiketopiperazines affords homochiral (S)-α-amino acids in excellent yield.
Poststatin, a new inhibitor of prolyl endopeptidase. VII. N-cycloalkylamide analogues
Tsuda, Makoto,Muraoka, Yasuhiko,Nagai, Machiko,Aoyagi, Takaaki,Takeuchi, Tomio
, p. 909 - 920 (2007/10/03)
Poststatin analogues containing (S)-2-oxo-2-(2-pyrrolidinyl)acetyl moiety in P1 were synthesized and examined for their inhibitory activity against prolyl endopeptidase and cathepsin B in vitro. Introduction of non-peptidyl cycloalkylamine component in P'1 was effective and P3-acyl groups must be widely modifiable for prolyl endopeptidase inhibition. Acyl-L-phenylalanyl-(S)-2-oxo-2-(2-pyrrolidinyl)acetyl-cycloalkylamide type compounds showed IC50 value of nano to subnano g/ml as prolyl endopeptidase inhibitor and were shown no significant inhibitory activities against cathepsin B, a cysteine protease.