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N-glucuronidation: the human element

Metabolite Tales Blog

To curb glucuronidation at that position a gem-dimethyl group was incorporated which not only boosted metabolic stability, but also resulted in increased potency of the final lead compound. Paine and Aleksandra Galetin (2014). Drug Metabolism and Disposition 42 (4) 650-664; [link]. [2] Polli, Mary F. J Pharm Biomed Anal.

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Efficient trajectories

Molecular Design

Design decisions in lead optimization are typically supported by assays for a range of properties such as solubility, permeability, metabolic stability and off-target activity as well as pharmacokinetic studies.