Bioorganic & Medicinal Chemistry Letters 2009-08-15

From lead to preclinical candidate: optimization of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV.

Sonja Nordhoff, Meritxell López-Canet, Barbara Hoffmann-Enger, Stephan Bulat, Silvia Cerezo-Gálvez, Oliver Hill, Claudia Rosenbaum, Christian Rummey, Meinolf Thiemann, Victor G Matassa, Paul J Edwards, Achim Feurer

Index: Bioorg. Med. Chem. Lett. 19(16) , 4818-23, (2009)

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Abstract

A series of highly potent and selective inhibitors of DPP-4 was optimized for ADMET properties. The effort resulted in the discovery of inhibitor 1g, that exhibits excellent efficacy in an oral glucose tolerance test and an attractive pharmacokinetic profile.

Related Compounds

  • DL-Homophenylalan...
  • l-homophenylalanin...

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