title: NEW RENIN-INHIBITORS--STABILITY AND ACTIVITY DETERMINATION. PART III.
abstract: A series of new four potential renin inhibitors containing pseudodipeptides were synthesized. Stability for all compounds (1-4) in homogenates of liver, kidney, lung and in serum, gastric, intestinal juice and in the presence of α-chymotrypsin was determined. Compound 1 was unstable, compounds 2, 3 were stable, compound 4 was partly unstable, (liver and kidney homogenates, (α-chymotrypsin solution). Inhibitory activity of the compounds was measured in vitro by HPLC determination of lowering concentration of substrate (angiotensinogen) in the presence of renin and the potential renin inhibitor (compounds 1-4). Compound 1, 2, 3 and 4 showed inhibitory activity (1.7 x 10(-6), 9.6 x 10(-7), 1.05 x 10(-9) and 1.31 x 10(-7)M, respectively).
authors.forename: Dorota
authors.initials: D
authors.lastname: Marszałek
authors.forename: Anna
authors.initials: A
authors.lastname: Goldnik
authors.forename: Iwona
authors.initials: I
authors.lastname: Winiecka
authors.forename: Paweł
authors.initials: P
authors.lastname: Jaworski
authors.forename: Aleksander P
authors.initials: AP
authors.lastname: Mazurek
mesh_terms: D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D002918:Chymotrypsin / Q000378:metabolism; D004355:Drug Stability; D005750:Gastric Juice / Q000378:metabolism; D006801:Humans; D007419:Intestinal Secretions / Q000378:metabolism; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D008168:Lung / Q000378:metabolism; D015394:Molecular Structure; D010455:Peptides / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D012083:Renin / Q000378:metabolism; D013329:Structure-Activity Relationship; D013678:Technology, Pharmaceutical / Q000379:methods; D000092502:Renin Inhibitors
chemical_list: D002918:Chymotrypsin; D010455:Peptides; D011480:Protease Inhibitors; D012083:Renin; D000092502:Renin Inhibitors; C117608:alpha-chymotrypsin