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3 results on '"Angelina Wallier"'

1. Aminomethylpyridines as DPP-IV inhibitors

Author

Matthias Steger, Daniel Zimmerli, Silja Weber, Bernd-Michael Loeffler, Stéphane Kritter, Markus Boehringer, Jens-Uwe Peters, Peter Weiss, and Angelina Wallier

Subjects
animal structures, Stereochemistry, Pyridines, Dipeptidyl Peptidase 4, Clinical Biochemistry, Pharmaceutical Science, Biochemistry, Chemical synthesis, Hydrocarbons, Aromatic, Inhibitory Concentration 50, Structure-Activity Relationship, Drug Discovery, Amines, Enzyme Inhibitors, Molecular Biology, Cells, Cultured, chemistry.chemical_classification, Dpp iv inhibitors, biology, Organic Chemistry, General Medicine, In vitro, Enzyme, chemistry, Diabetes Mellitus, Type 2, Enzyme inhibitor, Benzene derivatives, biology.protein, Molecular Medicine
Abstract

In a novel series of DPP-IV inhibitors, a large increase of inhibitory activity was achieved by optimisation of aromatic substituents and conformational restriction.

Published
2004

2. An aminomethylpyrimidine DPP-IV inhibitor with improved properties

Author

Bernd-Michael Loeffler, Aranka Müller, Jens-Uwe Peters, Miklos Csato, Markus Boehringer, Fabienne Ricklin, Daniel Hunziker, Holger Fischer, Silja Weber, Manfred Kansy, Angelina Wallier, Sonia Poli, and Stéphane Kritter

Subjects
Stereochemistry, Dipeptidyl Peptidase 4, Clinical Biochemistry, Pharmaceutical Science, Ether, Lipidoses, Biochemistry, Chemical synthesis, chemistry.chemical_compound, Inhibitory Concentration 50, Drug Discovery, Amphiphile, Cytochrome P-450 CYP3A, Cytochrome P-450 Enzyme Inhibitors, Humans, Protease Inhibitors, Amines, Molecular Biology, Phospholipidosis, chemistry.chemical_classification, biology, CYP3A4, Molecular Structure, Organic Chemistry, In vitro, Enzyme, Pyrimidines, chemistry, Enzyme inhibitor, biology.protein, Molecular Medicine
Abstract

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.

Published
2004

3. Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents

Author

Jens-Uwe Peters, Bernd-Michael Loeffler, Bernd Kuhn, Stéphane Kritter, Peter Weiss, Silja Weber, Michael Hennig, Angelina Wallier, and Markus Boehringer

Subjects
Molecular model, Stereochemistry, Adenosine Deaminase, Clinical Biochemistry, Pharmaceutical Science, Ether, Electrophilic aromatic substitution, Biochemistry, Chemical synthesis, Dipeptidyl peptidase, chemistry.chemical_compound, Drug Discovery, Hydrolase, Adenosine Deaminase Inhibitors, Protease Inhibitors, Molecular Biology, Glycoproteins, Dpp iv inhibitors, biology, Chemistry, Organic Chemistry, Active site, General Medicine, Pyrimidines, Enzyme inhibitor, biology.protein, Molecular Medicine
Abstract

The influence of aromatic substitution on a newly discovered class of inhibitors of dipeptidyl peptidase IV was investigated. A 10(5)-fold increase in potency was achieved by the optimization of aromatic substituents in a parallel chemistry program. The observed SAR could be explained by an X-ray structure of the protein-ligand complex.

Published
2003

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