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Bioprecursors and Bioactivation Mechanisms

Bioprecursors result from molecular modification of active principles, leading to new compounds metabolized into expected active agents through oxidation, reduction, and other processes. Learn about bioactivation processes in various substances such as cyclophosphamide, diazepam, and more.

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Bioprecursors and Bioactivation Mechanisms

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  1. Bioprecursors • Bioprecursors result from a molecular modification of the active principle itself. This modification generates a new compound, able to be a substrate for the metabolizing enzymes (often, oxidation and reduction). The metabolite being the expected active principle.

  2. (i) Bioactivation • Hydroxylation of cyclophosphamide (anticancer agent) followed by metabolite decomposition converts the prodrug to the cytotoxic phosphoramide mustard. • the activation involved oxidative dealkylation followed by a spontaneous hydrolysis to the parent active nitrogen mustard.

  3. (ii) N-dealkylation • Diazepam is converted to the active metabolite by N-dealkylation

  4. (iii) O-dealkylation • The analgesic phenacetin acts in the form of its dealkylated derivative, acetaminophen

  5. (iv) Reduction • The non-steroidal anti-inflammatory drug sulindac is reduced in vivoto the active form

  6. (v) Selective bioactivation • The insecticide, Malathion (acetylcholinesterase inhibitor), is desulfurized selectively to the toxic Malaoxon, but only by insect and not mammalian enzymes, Malathion is, therefore, Relatively non-toxic to mammals.

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