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Bioprecursors

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.

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Bioprecursors

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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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