110613-58-6Relevant academic research and scientific papers
HETEROCYCLIC RENIN INHIBITORS
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, (2008/06/13)
A renin inhibiting compound of the formula: STR1 wherein A is a substituent; R 1 is loweralkyl, loweralkenyl, alkoxyalkyl, [(alkoxy) alkoxy]alkyl, alkoxycarbonylalkyl, carboxyalkyl, (thioalkoxy) alkyl, benzyl or heterocyclic ring substituted methyl; R 2 i
Renin Inhibitors Based on Novel Dipeptide Analogues. Incorporation of the Dehydrohydroxyethylene Isostere at the Scissile Bond
Kempf, Dale J.,Lara, Ed de,Stein, Herman H.,Cohen, Jerome,Plattner, Jacob J.
, p. 1978 - 1983 (2007/10/02)
The design and synthesis of renin inhibitors that incorporate the novel dipeptide isostere (4S,5S)-5-amino-6-cyclohexyl-4-hydroxyhex-1-ene-2-carboxylic acid as a transition-state analogue are described.Titanium-promoted condensation of dilithiated N-alkylmethacrylamides with protected amino aldehydes results in efficient preparation of protected dipeptide analogues 7 and 8.Incorporation of 7 into the partial sequence of angiotensinogen affords potent in vitro inhibitors of human renin.Further chemical manipulation of the unsaturated amide moiety allows the study of structure-activity relationships in both the P1' and P2' sites.Details of the syntheses, stereochemical determinations, and in vitro renin inhibition are presented.
