Molecular toxicology and the medicinal chemist

Farmaco

Volumn 53, Issue 4, 1998, Pages 287-291

  Testa, Bernard ^a   Mayer, Joachim ^a  

^a UNIVERSITY OF LAUSANNE   (Switzerland)

Author keywords

Adducts; Conjugation; Detoxication; Functionalization; Reactive metabolites; Toxication

Indexed keywords

XENOBIOTIC AGENT;

BIOTRANSFORMATION; CONFERENCE PAPER; CONJUGATION; DETOXIFICATION; DRUG DESIGN; DRUG METABOLISM; DRUG RESEARCH; ENZYME SPECIFICITY; LIPOPHILICITY; METABOLITE; NONHUMAN; PHYSICAL CHEMISTRY; TOXICITY;

BIOTRANSFORMATION; CHEMISTRY, PHARMACEUTICAL; SUBSTRATE SPECIFICITY; XENOBIOTICS;

EID: 0031870694     PISSN: 0014827X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-827X(98)00012-3     Document Type: Conference Paper

References (15)

1. B. Testa, The Metabolism of Drugs and Other Xenobiotics - Biochemistry of Redox Reactions, 1955, Academic Press, London, 1955, p. 471.
2. B. Testa, Drug metabolism, in: M.E. Wolff (ed.), Burger's Medicinal Chemistry and Drug Discovery, Wiley-Interscience, New York, 5th edn., 1955, pp. 129-180.
3. C.G. Wermuth, B. Testa, Biotransformation reactions, in: C.G. Wermuth (ed.), The Practice of Medicinal Chemistry, Academic Press, London, 1996, pp. 615-641.
4. B. Walther, P. Vis, A. Taylor, Lipophilicity of metabolites and its role in biotransformation, in: V. Pliska, B. Testa, H. van de Waterbeemd (eds.), Lipophilicity in Drug Action and Toxicology, VCH, Weinheim, 1996, 253-261.
5. Caron G., Carrupt P.A., Testa B., Ermondi G., Gasco A. Insight into the lipophilicity of the aromatic N-oxide moiety. Pharm. Res. 13:1996;1186-1190.
6. Caron G., Gaillard P., Carrupt P.A., Testa B. Lipophilicity behavior of model and medicinal compounds containing a sulfide, sulfoxide or sulfone moiety. Helv. Chim. Acta. 80:1997;449-462.
7. Gaillard P., Carrupt P.A., Testa B. The conformation-dependent lipophilicity of morphine glucuronides as calculated from their molecular lipophilicity potential. Bioorg. Med. Chem. Lett. 4:1994;737-742.
8. Giroud Y., Carrupt P.A., Gaillard P., Testa B., Dickinson R.G. Intrinsic and intramolecular lipophilicity effects in O-glucuronides. Helv. Chim. Acta. 81:1998;330-341.
9. Testa B., Caldwell J. Prodrugs revisited: the ad hoc approach as a complement to ligand design. Med. Res. Rev. 16:1996;233-241.
10. Gangwar S., Pauletti G.M., Wang B., Siahaan T.J., Stella V.J., Borchardt R.T. Prodrug strategies to enhance the intestinal absorption of peptides. Drug Discovery Today. 2:1997;148-155.
11. Smith D.A., Ackland M.J., Jones B.C. Properties of cytochrome P450 isoenzymes and their substrates. Part 1. Active site characteristics Drug Discovery Today. 2:1997;406-414.
12. D.A. Smith, M.J. Ackland, B.C. Jones, Properties of cytochrome P450 isoenzymes and their substrates. Part 2. Properties of cytochrome P450 substrates, Drug Discovery Today 2 (1997) 479-486.
13. J. Mayer, B. Testa, Stereoselectivity in metabolic reactions of toxication and detoxication, in: P.G. Welling, L.P. Balant (eds.), Pharmacokinetics of Drugs, Springer, Berlin, 1994, pp. 209-231.
14. Korfmacher W.A., Cox K.A., Bryant M.S., Veals J., Ng K., Watkins R., Lin C.C. HPLC-API/MS/MS: a powerful tool for integrating drug metabolism into the drug discovery process. Drug Discovery Today. 2:1997;532-537.
15. J.M. Mayer, B. Testa, M. Roy-de Vos, C. Audergon, J.-C. Etter, Interactions between the in vitro metabolism of xenobiotics and fatty acids. The case of ibuprofen and other chiral profens, Arch. Toxicol. (Suppl. 17) (1995) 499-513.