Bioprecursor Prodrugs: Molecular Modification of the Active Principle

Author(s): Ganesh R. Kokil, Prarthana V. Rewatkar.

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 10 , Issue 14 , 2010

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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

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Article Details

VOLUME: 10
ISSUE: 14
Year: 2010
Page: [1316 - 1330]
Pages: 15
DOI: 10.2174/138955710793564179
Price: $58

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