Bioprecursor Prodrugs: Molecular Modification of the Active Principle

Ganesh      R. Kokil; Prarthana      V. Rewatkar

Abstract

A large number of therapeutic medications have undesirable properties that may generate pharmacological, pharmaceutical, or pharmacokinetic barriers in clinical drug applications. Metabolism of drugs by Phase-I & Phase-II metabolic pathways for possibility of active metabolites, which could in turn useful for rational designing of bioprecursor prodrugs of the active principle of interest. This review summarizes various approaches & development of drugs, namely bioprecursor prodrugs and active metabolites related to bioprecursor prodrugs.

Keywords: Bioprecursor prodrugs, active metabolites, oxidative activation, glucuronic acid conjugation, bioreductive alkylation, prodrugs, proagent, O-demethylated metabolite of phenacetin, phenacetin, OXIDATION, Cytochrome P450 Mono-Oxygenase, NADPH-CYP reductase, CYP enzymes, xenobiotics, Flavin-Containing Monooxygenase System, FMO family, lipophilic compounds, Monoamine Oxidase, neurotransmitter amines, clorgyline, serotonin, L-deprenyl, oxidize dopamine, tyramine, octopamine, hydrogen peroxide, NADPH-cytochrome P450 reductase, NADH-putidaredoxin reductase, Nabumetone, Dexpathenol, 3-pyridine methanol, mitomycin, nitrogen mustard, omeprazole, Sulindac, SAH 51-641, acyl CoA ligase, gluconeogenesis, aroylpropionic acids, aryl acetic acid, aroylpropionic acid, bucloxic acid, indomethacin, Idoxuridine, thymidine kinase, Methyltransferase, Glutathione S-Transferases, Sulfotransferases System, N-Acetyltransferases System, UDP-Glucuronosyltransferases, UDP, Minoxidil, paclitaxel