Small changes for long term impact : optimization of structure kinetic properties : a case of CCR2 antagonists

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Small changes for long term impact : optimization of structure kinetic properties : a case of CCR2 antagonists

Title: Small changes for long term impact : optimization of structure kinetic properties : a case of CCR2 antagonists
Author: Vilums, Maris
Publisher: Leiden Academic Centre for Drug Research (LACDR), Faculty of Science, Leiden University
Issue Date: 2014-11-20
Keywords: Structure-Kinetics Relationships
Long Residence Time
CCR2 antagonists
Indane
Inflammatory diseases
Abstract: This thesis focuses on a new approach in drug discovery, the so-called drug-target residence time. Next to more traditional drug discovery efforts, which are based on structure-affinity relationships, this thesis describes the use of an additional parameter – the structure-kinetic relationships. Knowledge of this additional parameter at the early stages of drug discovery may help the pharmaceutical industry to generate better drug candidates. Additionally, it could save big expenses in the later stages of drug discovery by minimizing the attrition rate of drug candidates due to efficacy problems. In more detail, this thesis focuses on the synthesis of new high affinity and long residence time small molecule antagonists for the chemokine receptor CCR2 - a potential target for the treatment of various inflammatory diseases.
Description: Promotor: A.P. IJzerman, Co-Promotor: L.H. Heitman
With Summary in Dutch
Faculty: Faculteit der Wiskunde en Natuurwetenschappen
Citation: Vilums, M., 2014, Doctoral Thesis, Leiden University
Handle: http://hdl.handle.net/1887/29811
 

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