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

Promotor: Prof.dr. A. P. IJzerman, Co-Promotor: Dr. L.H. Heitman

M. Viļums
20 November 2014
Thesis in Leiden Repository

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.

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