CYP1A1 and CYP1B1-mediated biotransformation of the antitrypanosomal methamidoxime prodrug DB844 forms novel metabolites through intramolecular rearrangement

DB844 (CPD-594-12), N-methoxy-6-{5-[4-(N-methoxyamidino)phenyl]-furan-2-yl}-nicotinamidine, is an oral prodrug that has shown promising efficacy in both mouse and monkey models of second stage human African trypanosomiasis. However, gastrointestinal (GI) toxicity was observed with high doses in a ve...

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Main Authors: Ju, Wujian, Yang, Sihyung, Ansede, John H., Stephens, Chad E., Bridges, Arlene S., Voyksner, Robert D., Ismail, Mohamed A., Boykin, David W., Tidwell, Richard R., Hall, James Edwin, Wang, Michael Zhuo
Formato: Artigo
Idioma:Inglês
Publicado em: 2013
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3865069/
https://ncbi.nlm.nih.gov/pubmed/24186380
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/jps.23765
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