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Introduction to Human Cytochrome P450 Superfamily
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Besides endogenous substrates, CYP4F enzymes are involved in the metabolism of xenobiotics including some drugs, but it is considered that this family seems to play a minor role in drug metabolism. CYP4F11 metabolizes erythromycin and ethylmorphine (Kalsotra et al. 2004), and 4F12 metabolizes ebastine with contribution from 2J2 (Hashizume et al. 2002). The new immunomodulatory agent used for the treatment of relapsing multiple sclerosis, fingolimod (FTY720; 2-amino-2-[2-(4-octylphenyl)ethyl]-1,3-propanediol), is eliminated predominantly by CYP4F2 or 4F3B-mediated ω-hydroxylation of the aliphatic chain (Jin et al. 2011). CYP4F2 and 4F3B also catalyze the O-demethylation of the antitrypanosomal methamidoxime prodrugs pafuramidine (DB289; 2,5-bis(4-amidinophenyl)furan-bis-O-methylamidoxime), DB844, and DB868 (Ju et al. 2014; M.Z. Wang et al. 2006).
Synthesis, anti-bacterial and anti-protozoal activities of amidinobenzimidazole derivatives and their interactions with DNA and RNA
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Andrea Bistrović, Luka Krstulović, Ivana Stolić, Domagoj Drenjančević, Jasminka Talapko, Martin C. Taylor, John M. Kelly, Miroslav Bajić, Silvana Raić-Malić
Besides anti-bacterial activity, benzimidazole containing compounds have shown good anti-protozoal potency45–49. Human African trypanosomiasis (HAT), also known as sleeping sickness, is a fatal parasitic disease caused by two subspecies of Trypanosoma brucei. It has been estimated that over 50 million people are at risk of infection with HAT in more than 30 African countries, and there remains a clear need to develop new, safer, and more affordable agents to combat this fatal infection50. The efficacy of diarylamidines, such as pentamidine51, berenyl52 and its orally active prodrug pafuramidine53 (Figure 2), in the treatment of protozoal diseases, especially trypanosomiasis, has been known for many years.