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Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a structurally modified phenylalanine residue to impart proteolytic stability.

Abstract：

:A series of renin inhibitors have been prepared and evaluated for their susceptibility to cleavage by the serine protease chymotrypsin. The compounds were designed by consideration of the structural requirements in the active-site region of renin and chymotrypsin. By systematic alteration of the P3 phenylalanine residue, compounds with varying degrees of renin inhibitory potency and chymotrypsin susceptibility were obtained. Selected analogues from this group were examined in vivo for both their hypotensive effects and metabolic patterns.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Plattner JJ,Marcotte PA,Kleinert HD,Stein HH,Greer J,Bolis G,Fung AK,Bopp BA,Luly JR,Sham HL

doi

10.1021/jm00120a006

subject

Has Abstract,Author List Incomplete

pub_date

1988-12-01 00:00:00

pages

2277-88

issue

12

eissn

0022-2623

issn

1520-4804

journal_volume

31

pub_type

杂志文章

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