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Many years of work have been invested in the identification of potent and selective COX-2 inhibitors for the treatment of chronic inflammatory pain. One issue faced by workers is the balance between the lipophilicity required for potent enzyme inhibition and the physical properties necessary for drug absorption and distribution in vivo. Frequently approaches to reduce lipophilicity through introduction of polar functionality is hampered by highly challenging chemistry to prepare key molecules. We have complemented traditional synthetic chemistry with a biotransformations approach which efficiently provided access to an array of key target molecules.

Original publication

DOI

10.1016/j.bmcl.2009.02.089

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

01/08/2009

Volume

19

Pages

4509 - 4514

Keywords

Biotransformation, Chemistry, Pharmaceutical, Cyclooxygenase 2, Cyclooxygenase 2 Inhibitors, Drug Design, Humans, Inflammation, Inhibitory Concentration 50, Models, Chemical, Molecular Structure, Structure-Activity Relationship