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Items: 1 to 20 of 104

1.
2.

Novel metabolic bioactivation mechanism for a series of anti-inflammatory agents (2,5-diaminothiophene derivatives) mediated by cytochrome p450 enzymes.

Hu Y, Yang S, Shilliday FB, Heyde BR, Mandrell KM, Robins RH, Xie J, Reding MT, Lai Y, Thompson DC.

Drug Metab Dispos. 2010 Sep;38(9):1522-31. doi: 10.1124/dmd.110.032581. Epub 2010 Jun 7.

3.

Bioactivation of isothiazoles: minimizing the risk of potential toxicity in drug discovery.

Teffera Y, Choquette D, Liu J, Colletti AE, Hollis LS, Lin MH, Zhao Z.

Chem Res Toxicol. 2010 Nov 15;23(11):1743-52. doi: 10.1021/tx100208k. Epub 2010 Sep 8.

PMID:
20825217
4.
5.
6.

Identification of the thiophene ring of methapyrilene as a novel bioactivation-dependent hepatic toxicophore.

Graham EE, Walsh RJ, Hirst CM, Maggs JL, Martin S, Wild MJ, Wilson ID, Harding JR, Kenna JG, Peter RM, Williams DP, Park BK.

J Pharmacol Exp Ther. 2008 Aug;326(2):657-71. doi: 10.1124/jpet.107.135483. Epub 2008 May 1.

7.

Bioactivation of substituted thiophenes including α-chlorothiophene-containing compounds in human liver microsomes.

Chen W, Caceres-Cortes J, Zhang H, Zhang D, Humphreys WG, Gan J.

Chem Res Toxicol. 2011 May 16;24(5):663-9. doi: 10.1021/tx100386z. Epub 2011 Apr 13.

PMID:
21417487
8.

Mechanism-based inactivation of human recombinant P450 2C9 by the nonsteroidal anti-inflammatory drug suprofen.

O'Donnell JP, Dalvie DK, Kalgutkar AS, Obach RS.

Drug Metab Dispos. 2003 Nov;31(11):1369-77.

9.

Reversible time-dependent inhibition of cytochrome P450 enzymes by duloxetine and inertness of its thiophene ring towards bioactivation.

Chan CY, New LS, Ho HK, Chan EC.

Toxicol Lett. 2011 Oct 30;206(3):314-24. doi: 10.1016/j.toxlet.2011.07.019. Epub 2011 Aug 5.

PMID:
21839818
12.

NADPH-dependent covalent binding of [3H]paroxetine to human liver microsomes and S-9 fractions: identification of an electrophilic quinone metabolite of paroxetine.

Zhao SX, Dalvie DK, Kelly JM, Soglia JR, Frederick KS, Smith EB, Obach RS, Kalgutkar AS.

Chem Res Toxicol. 2007 Nov;20(11):1649-57. Epub 2007 Oct 2.

PMID:
17907785
13.

Bioactivation of benzylamine to reactive intermediates in rodents: formation of glutathione, glutamate, and peptide conjugates.

Mutlib AE, Dickenson P, Chen SY, Espina RJ, Daniels JS, Gan LS.

Chem Res Toxicol. 2002 Sep;15(9):1190-207.

PMID:
12230413
14.

Metabolism and bioactivation of 3-methylindole by human liver microsomes.

Yan Z, Easterwood LM, Maher N, Torres R, Huebert N, Yost GS.

Chem Res Toxicol. 2007 Jan;20(1):140-8.

PMID:
17226936
15.

A rational chemical intervention strategy to circumvent bioactivation liabilities associated with a nonpeptidyl thrombopoietin receptor agonist containing a 2-amino-4-arylthiazole motif.

Kalgutkar AS, Driscoll J, Zhao SX, Walker GS, Shepard RM, Soglia JR, Atherton J, Yu L, Mutlib AE, Munchhof MJ, Reiter LA, Jones CS, Doty JL, Trevena KA, Shaffer CL, Ripp SL.

Chem Res Toxicol. 2007 Dec;20(12):1954-65. Epub 2007 Oct 13.

PMID:
17935300
16.
17.

Evidence for the bioactivation of zomepirac and tolmetin by an oxidative pathway: identification of glutathione adducts in vitro in human liver microsomes and in vivo in rats.

Chen Q, Doss GA, Tung EC, Liu W, Tang YS, Braun MP, Didolkar V, Strauss JR, Wang RW, Stearns RA, Evans DC, Baillie TA, Tang W.

Drug Metab Dispos. 2006 Jan;34(1):145-51. Epub 2005 Oct 26.

18.
19.

First evidence that cytochrome P450 may catalyze both S-oxidation and epoxidation of thiophene derivatives.

Dansette PM, Bertho G, Mansuy D.

Biochem Biophys Res Commun. 2005 Dec 9;338(1):450-5. Epub 2005 Aug 22.

PMID:
16137656
20.

Bioactivation of sitaxentan in liver microsomes, hepatocytes, and expressed human P450s with characterization of the glutathione conjugate by liquid chromatography tandem mass spectrometry.

Erve JC, Gauby S, Maynard JW Jr, Svensson MA, Tonn G, Quinn KP.

Chem Res Toxicol. 2013 Jun 17;26(6):926-36. doi: 10.1021/tx4001144. Epub 2013 May 30.

PMID:
23721565

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