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An aminomethylpyrimidine DPP-IV inhibitor with improved properties

2004; Elsevier BV; Volume: 14; Issue: 13 Linguagem: Inglês

10.1016/j.bmcl.2004.04.048

1464-3405

Jens‐Uwe Peters, Daniel Hunziker, Holger Fischer, Manfred Kansy, Silja Weber, Stéphane Kritter, Aranka Müller, Angelina Wallier, Fabienne Ricklin, Markus Boehringer, Sonia Poli, M. Csató, Bernd‐Michael Loeffler,

Peptidase Inhibition and Analysis

A recently identified DPP-IV inhibitor (1) was found to induce phospholipidosis and to inhibit CYP3A4. A small series of less lipophilic and less amphiphilic analogues was synthesized in an effort to overcome these issues. One compound from this series was equipotent to 1, did not induce phospholipidosis and showed a reduced CYP3A4 inhibition.