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  • Title: Lead optimization strategies as part of a drug metabolism environment.
    Author: Korfmacher WA.
    Journal: Curr Opin Drug Discov Devel; 2003 Jul; 6(4):481-5. PubMed ID: 12951811.
    Abstract:
    The rapid increase in the rate at which new chemical entities can be synthesized by medicinal chemists and tested in vitro for potency using high-throughput screening has provided opportunities for lead selection and optimization of thousands of compounds in major pharmaceutical companies. This opportunity coincides with the realization that drug metabolism input at the lead optimization stage is crucial for the development of compounds, with increased likelihood of success when tested in preclinical safety studies and in phase I trials. This has led to new discovery and optimization paradigms, in which drug metabolism is playing an important role.
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