125816-10-6Relevant articles and documents
Renin inhibitors
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, (2008/06/13)
A renin inhibiting compound of the formula: STR1 wherein X is O, NH or S and G is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof; with the proviso that the compound is not N-(3-(4-M
Nonpeptide renin inhibitors with good intraduodenal bioavailability and efficacy in dog
Boyd,Fung,Baker,Mantei,Stein,Cohen,Barlow,Klinghofer,Wessale,Verburg,Polakowski,Adler,Calzadilla,Kovar,Yao,Hutchins,Denissen,Grabowski,Cepa,et al.
, p. 2991 - 3007 (2007/10/02)
The aim of this study was the discovery of nonpeptide renin inhibitors with much improved oral absorption, bioavailability, and efficacy, for use as antihypertensive agents. Our prior efforts led to the identification of A- 74273 [1, R = 3-(4-morpholino)p
The stereospecific preparation of a hydroxyethylene isostere precursor via a novel piperidine-2,5-dione template
Plata,Leanna,Morton
, p. 3623 - 3626 (2007/10/02)
Hydroxyethylene isostere precursor 2 was synthesized by stereochemical manipulation of a novel ketolactam 'template'. The final product was prepared in very high enantiomeric purity, in 23% overall yield from L-phenylalanine.
Synthesis of renin inhibitors possessing hydroxyethylene isostere residue from 3,4,6-tri-O-acetyl-D-glucal via lactone precursor
Shiozaki,Kobayashi,Hata,Furukawa
, p. 2785 - 2800 (2007/10/02)
Syntheses of precursors for renin inhibitors possessing hydroxyethylene isostere residue from 2,4,6-tri-O-acetyl-D-glucal via lactone precursor is described . This route makes it possible to synthesize analogues with various substituents at C-2 and C-5 of
A Stereoselective Synthesis of Hydroxyethylene and erythro-Dihydroxyethylene Dipeptide Isosteres: A Facial Selective anti-Aldol Reaction
Rosenberg, Saul H.,Boyd, Steven A.,Mantei, Robert A.
, p. 6507 - 6508 (2007/10/02)
A Lewis-acid catalyzed anti-aldol reaction of aldehyde 4 afforded diol 6a (95percent de).Aminolysis of the corresponding β-lactone provided erythro-dihydroxyethylene dipeptide isostere 2 while the lactone-protected hydroxyethylene dipeptide isostere 3 was obtained through selective deoxygenation and acidic deprotection. Key words: hydroxyethylene isostere; anti-aldol; aspartic proteinase; renin inhibitor; facial selective
1,2,4-Triazolopyrazine Derivatives with Human Renin Inhibitory Activity. 2. Synthesis, Biological Properties and Molecular Modeling of Hydroxyethylene Isostere Derivatives
Bradbury, Robert H.,Major, John S.,Oldham, Alec A.,Rivett, Janet E.,Roberts, David A.,et al.
, p. 2335 - 2342 (2007/10/02)
A series of inhibitors of human renin have been synthesized, derived from combination of a 2-(8-propyl-6-pyridin-3-yl-1,2,4-triazolopyrazin-3-yl)-3-pyridin-3-ylpropionic acid moiety 6c with the hydroxyethylene isostere of the scissile amide bond (2
AN EFFICIENT SYNTHESIS OF THE γ-LACTONE CORRESPONDING TO A HYDROXYETHYLENE DIPEPTIDE ISOSTERE USING STEREOSELECTIVE BROMOLACTONISATION OF A CHIRAL ACYLOXAZOLIDINONE
Bradbury, Robert H.,Revill, John M.,Rivett, Janet E.,Waterson, David
, p. 3845 - 3848 (2007/10/02)
An efficient synthetic route is described to the γ-lactone 11 corresponding to the dipeptide isostere (2S,4S,5S)-5-amino-6-cyclohexyl-4-hydroxy-2-isopropylhexanoic acid, in which stereochemical control is achieved by participation of chiral acyloxazolidinone 6 in a stereoselective bromolactonisation reaction.
SYNTHESIS OF THE LACTONE PRECURSOR TO HYDROXYETHYLENE DIPEPTIDE ISOSTERE FROM 3,4,6-TRI-O-ACETYL-D-GLUCAL
Shiozaki, Masao,Hata, Tadashi,Furukawa, Youji
, p. 3669 - 3670 (2007/10/02)
(2S,4S,5S)-5-Amino-6-cyclohexyl-4-hydroxy-2-isopropyl hexanoic acid lactone (5) was synthesized from 3,4,6-tri-O-acetyl-D-glucal in an efficient manner.
