Category Archives: Conjugation Reactions

Boronic Acid-Containing Proteasome Inhibitors: Alert to Potential Pharmaceutical Bioactivation CRT 2013

Posted on April 25, 2013 by admetchemist

Li. A. C. et al. Chem. Res. Toxicol., 2013, 26 (4), pp 608–615

Posted in Boronic acid, Bortezomib, Glutathione (GSH) Adducts, Imine amide, Millennium | Tagged , , | Leave a comment

Central Nervous System Disposition and Metabolism of Fosdevirine (GSK2248761), a Non-Nucleoside Reverse Transcriptase Inhibitor: An LC-MS and Matrix-Assisted Laser Desorption/Ionization Imaging MS Investigation into Central Nervous System Toxicity CRT 2013

Posted on January 21, 2013 by admetchemist

Castellino, S., et al. Chem. Res. Toxicol., 2013, 26 (2), pp 241–251

Posted in Blood Brain Barrier, CNS, Company, Conjugation Reactions, Drug Safety, Fosdevirine, GSK, GST, MALDI Imaging | Tagged , , , | Leave a comment

In Vitro Biotransformation Studies of 2‐Oxo-clopidogrel: Multiple Thiolactone Ring-Opening Pathways Further Attenuate Prodrug Activation CRT 2012

Posted on January 2, 2013 by admetchemist

Zhu, Y. and Zhou, J. Chem. Res. Toxicol., Article ASAP A new study on the biotransformation pathways of 2‐oxo-clopidogrel

Posted in Bioactivation, Biotransformation, BMS, Clopidogrel, Drug Metabolism, Glutathione (GSH) Adducts, Metabolite Identification (MetID), Metabolite Profiling, Thiophene | Tagged , , , , , | Leave a comment

Bioactivation of Isothiazoles: Minimizing the Risk of Potential Toxicity in Drug Discovery. Amgen CRT 2012

Posted on December 12, 2012 by admetchemist

Teffera, Y., et al. Chem. Res. Toxicol., 2010, 23 (11), pp 1743–1752  

Posted in 1A2, 2D6, 3A4, Bioactivation, Conjugation Reactions, Cytochrome P450, Glutathione (GSH) Adducts, Isothiazole | Tagged , | Leave a comment

Novel bioactivation mechanism of reactive metabolite formation from phenyl methyl-isoxazoles. Astrazeneca DMD 2012

Posted on December 11, 2012 by admetchemist

Bylund, J. et al. Drug Metab Dispos. 2012 Nov;40(11):2185-91

Posted in Bioactivation, Drug Metabolism, Enimine, Glutathione (GSH) Adducts, Reactive Intermediates | Tagged , , , , | Leave a comment

Reactive Intermediates Produced from the Metabolism of the Vanilloid Ring of Capsaicinoids by P450 Enzymes CRT 2012

Posted on November 26, 2012 by admetchemist

Reilly, C. A., et al. Chem. Res. Toxicol., Article ASAP

Posted in 1A2, 2C19, 2D6, 3A4, Bioactivation, Biotransformation, Capsaicinoids, Glutathione (GSH) Adducts, Human Liver Microsomes(HLM), P450 Phenotyping, Quinone, Quinone Methide, Reactive Intermediates | Tagged , , , , , , | Leave a comment

Bioactivation of the Epidermal Growth Factor Receptor Inhibitor Gefitinib: Implications for Pulmonary and Hepatic Toxicities CRT 2009

Posted on November 13, 2012 by admetchemist

Li, X., et al. Chem. Res. Toxicol., 2009, 22 (10), pp 1736–1742

Posted in Bioactivation, Biotransformation, Glutathione (GSH) Adducts, Quinone-imine | Tagged , , , , , , , | Leave a comment

Bioactivation of a Dihydropyrazole-1-carboxylic acid-(4-chlorophenyl amide) Scaffold to a Putative p-Chlorophenyl Isocyanate in Rat Liver Microsomes and In Vivo in Rats CRT 2008

Posted on October 29, 2012 by admetchemist

Chen, H., et al. Chem. Res. Toxicol., 2008, 21 (5), pp 1095–1106

Posted in Bioactivation, Biotransformation, Cytochrome P450, Glutathione (GSH) Adducts, Reactive Intermediates | Tagged , , , , , | Leave a comment

Chemical Toxicology of Reactive Intermediates Formed by the Glutathione-Dependent Bioactivation of Halogen-Containing Compounds by M.W. Anders CRT 2008

Posted on October 27, 2012 by admetchemist

Anders, M. W., Chem. Res. Toxicol., 2008, 21 (1), pp 145–159 A comprehensive review of bioactivation of halogen-containing compounds involving glutathione

Posted in Bioactivation, Glutathione (GSH) Adducts, Reactive Intermediates, Toxicity | Tagged , , , , | Leave a comment

Characterization of Novel Glutathione Adducts of a Non-Nucleoside Reverse Transcriptase Inhibitor, (S)-6-Chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-3,4-dihydro-2(1H)-quinazolinone (DPC 961), in Rats. Possible Formation of an Oxirene Metabolic Intermediate from a Disubstituted Alkyne by Abdul Mutlib CRT 2000

Posted on October 26, 2012 by admetchemist

Mutlib, A., et al. Chem. Res. Toxicol., 2000, 13 (8), pp 775–784 I would like to post a number of classical papers on MetID and biotransformation pathway elucidation. The first one is Abdul Mutlib’s work on an anti-HIV drug, DPC 961 published some years ago, using LC-MS, NMR and … Continue reading →

Posted in Biotransformation, Drug Metabolism, Glutathione (GSH) Adducts, Radioisotope Label, Reactive Intermediates | Tagged , , , , | Leave a comment