New renin inhibitors--stability and activity determination. Part I
A series of new six potential renin inhibitors containing pseudodipeptides were synthesized. Stability for all compounds (1-6) in homogenates of liver, kidney, lung and in serum, gastric, intestinal juice and in the presence of alpha-chymotrypsin was determined. Compound 5 was unstable, compound 6 was stable, other compounds were partly unstable, compound 2 was stable except kidney homogenate and compound 4 was stable except liver homogenate. 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 1-6). Compound 2, 4 and 6 showed inhibitory activity (1.4 x 10(-6), 5.2 x 10(-6), 1.5 x 10(-7) M, respectively). Other compounds (1, 3, 5) showed no inhibitory activity up to 10(-5) M.
Medienart: |
Artikel |
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Erscheinungsjahr: |
2014 |
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Erschienen: |
2014 |
Enthalten in: |
Zur Gesamtaufnahme - volume:71 |
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Enthalten in: |
Acta poloniae pharmaceutica - 71(2014), 4 vom: 04. Juli, Seite 545-53 |
Sprache: |
Englisch |
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Beteiligte Personen: |
Marszałek, Dorota [VerfasserIn] |
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Themen: |
Alpha-chymotrypsin |
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Anmerkungen: |
Date Completed 10.11.2014 Date Revised 25.11.2016 published: Print Citation Status MEDLINE |
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Förderinstitution / Projekttitel: |
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PPN (Katalog-ID): |
NLM242385087 |
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245 | 1 | 0 | |a New renin inhibitors--stability and activity determination. Part I |
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520 | |a A series of new six potential renin inhibitors containing pseudodipeptides were synthesized. Stability for all compounds (1-6) in homogenates of liver, kidney, lung and in serum, gastric, intestinal juice and in the presence of alpha-chymotrypsin was determined. Compound 5 was unstable, compound 6 was stable, other compounds were partly unstable, compound 2 was stable except kidney homogenate and compound 4 was stable except liver homogenate. 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 1-6). Compound 2, 4 and 6 showed inhibitory activity (1.4 x 10(-6), 5.2 x 10(-6), 1.5 x 10(-7) M, respectively). Other compounds (1, 3, 5) showed no inhibitory activity up to 10(-5) M | ||
650 | 4 | |a Journal Article | |
650 | 4 | |a Research Support, Non-U.S. Gov't | |
650 | 7 | |a Enzyme Inhibitors |2 NLM | |
650 | 7 | |a Chymotrypsin |2 NLM | |
650 | 7 | |a EC 3.4.21.1 |2 NLM | |
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700 | 1 | |a Goldnik, Anna |e verfasserin |4 aut | |
700 | 1 | |a Mazurek, Aleksander P |e verfasserin |4 aut | |
700 | 1 | |a Winiecka, Iwona |e verfasserin |4 aut | |
700 | 1 | |a Jaworskpi, Paweł |e verfasserin |4 aut | |
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