Physical Chemical Aspects of Drug Design: Isolipophilic Modification of Ibuprofen Metablites
Riebe, Michael T.
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It is hypothesized that the absence of biological activity in these metabolites is due to their significantly reduced lipophilicity relative to that typical for most NSAIDs. For present purposes, lipophilicity will be defined as the relative affinity of a molecule toward oils or water. To test this hypothesis, it was proposed that these metabolites be chemically modified (esterified) to achieve the same lipophilicity as the parent ibuprofen and then tested for biological activity. As metabolism of these proposed compounds would likely yield the same metabolites as ibuprofen (namely II and III), the toxicity of the new compounds should be minimal.