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Human African trypanosomiasis: pharmacological re‐engagement with a neglected disease
The challenges of chemotherapy for human African trypanosomiasis (HAT) are discussed, and the few drugs registered for use against the disease are unsatisfactory for a number of reasons.
Antiparasitic compounds that target DNA.
New Treatment Option for Second-Stage African Sleeping Sickness: In Vitro and In Vivo Efficacy of Aza Analogs of DB289
- T. Wenzler, D. Boykin, M. Ismail, J. Hall, R. Tidwell, R. Brun
- BiologyAntimicrobial Agents and Chemotherapy
- 20 July 2009
DB868 with oral and DB829 with parenteral application are potential candidates for further development of a second-stage African sleeping sickness drug.
Accumulation and Intracellular Distribution of Antitrypanosomal Diamidine Compounds DB75 and DB820 in African Trypanosomes
It is shown that DB75 and DB820 rapidly accumulate and strongly concentrate within trypanosomes, with intracellular concentrations over 15,000-fold higher than mouse plasma concentrations.
Cellular Effects of Reversed Amidines on Trypanosoma cruzi
The results show that the reversed amidines have promising activities against the relevant mammalian forms of T. cruzi and display high trypanocidal effects at very low doses.
Dications that target the DNA minor groove: compound design and preparation, DNA interactions, cellular distribution and biological activity.
- W. Wilson, Binh Nguyen, D. Boykin
- Biology, ChemistryCurrent medicinal chemistry. Anti-cancer agents
- 1 July 2005
It is clear that there are many ways for compounds to bind to k-DNA and exert specific effects on kinetoplast replication and/or transcription that are required to obtain an active compound.
Binding of 4',6-diamidino-2-phenylindole (DAPI) to GC and mixed sequences in DNA: intercalation of a classical groove-binding molecule
Aromatic diamidines as antiparasitic agents
- M. N. Soeiro, E. M. de Souza, C. E. Stephens, D. Boykin
- BiologyExpert opinion on investigational drugs
- 29 July 2005
The present aim is to review the current status of chemotherapy with these compounds against human parasitic infections and to explore the activity of aromatic diamidines against a widespread range of micro-organisms.
CYP4F Enzymes Are the Major Enzymes in Human Liver Microsomes That Catalyze the O-Demethylation of the Antiparasitic Prodrug DB289 [2,5-Bis(4-amidinophenyl)furan-bis-O-methylamidoxime]
- Michael Zhuo Wang, Janelle Y Saulter, J. Hall
- Biology, ChemistryDrug Metabolism and Disposition
- 1 December 2006
An in vitro metabolism study to characterize enzymes in human liver microsomes (HLMs) that catalyze the initial O-demethylation of DB289 confirmed that M1 formation is catalyzed by P450 enzymes, and indicated that members of the CYP4F subfamily biotransform not only endogenous compounds but also xenobiotics.
Antileishmanial Activities of Several Classes of Aromatic Dications
- J. Brendle, Abram Outlaw, K. Werbovetz
- Chemistry, BiologyAntimicrobial Agents and Chemotherapy
- 1 March 2002
The structure-activity relationships demonstrate the potent antileishmanial activity of several aromatic dications and provide valuable information for the future design and synthesis of more potent antiparasitic agents.