Design of potent and selective GSK3b inhibitors with acceptable safety profile and pharmacokinetics

Design of potent and selective GSK3b inhibitors with acceptable safety profile and pharmacokinetics

From potent and selective inhibitors of GSK3b displaying CYP1A2 inhibition and poor PK properties, mostly linked to metabolic instability and in vivo hydrolysis of the amide bond, we were able to obtain safe and orally available inhibitors with good half lives. AB:

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (7), p.2344-2349
Hauptverfasser: Lesuisse, Dominique, Tiraboschi, Gilles, Krick, Alain, Abecassis, Pierre-Yves, Dutruc-Rosset, Gilles, Babin, Didier, Halley, Frank, Chatreau, Fabienne, Lachaud, Sylvette, Chevalier, Alain, Quarteronet, Dominique, Burgevin, Marie-Claude, Amara, Celine, Bertrand, Philippe, Rooney, Thomas
Format: Artikel
Sprache:eng
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Zusammenfassung:From potent and selective inhibitors of GSK3b displaying CYP1A2 inhibition and poor PK properties, mostly linked to metabolic instability and in vivo hydrolysis of the amide bond, we were able to obtain safe and orally available inhibitors with good half lives. AB:
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.01.132