Substituted piperidines - highly potent renin inhibitors due to induced fit adaptation of the active site

The identification, synthesis and activity of a novel class of piperidine renin inhibitors is presented. The most active compounds show activities in the picomolar range and are among the most potent renin inhibitors ever identified. The identification, synthesis and activity of a totally novel clas...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 1999-05, Vol.9 (10), p.1397-1402
Hauptverfasser: Vieira, Eric, Binggeli, Alfred, Breu, Volker, Bur, Daniel, Fischli, Walter, Güller, Rolf, Hirth, Georges, Märki, Hans Peter, Müller, Marcel, Oefner, Christian, Scalone, Michelangelo, Stadler, Heinz, Wihelm, Maurice, Wostl, Wolfgang
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Sprache:eng
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Zusammenfassung:The identification, synthesis and activity of a novel class of piperidine renin inhibitors is presented. The most active compounds show activities in the picomolar range and are among the most potent renin inhibitors ever identified. The identification, synthesis and activity of a totally novel class of piperidine renin inhibitors is presented. The most active compounds show activities in the low picomolar range and are among the most potent renin inhibitors ever identified.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00195-X