Accumulation and Intracellular Distribution of Aromatic Diamidines in African Trypanosomes
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چکیده
....................................................................................45 Introduction .................................................................................46 Materials and Methods ....................................................................49 Results .......................................................................................55
منابع مشابه
Diphenyl furans and aza analogs: effects of structural modification on in vitro activity, DNA binding, and accumulation and distribution in trypanosomes.
Human African trypanosomiasis is a devastating disease with only a few treatment options, including pentamidine. Diamidine compounds such as pentamidine, DB75, and DB820 are potent antitrypanosomal compounds. Previous investigations have shown that diamidines accumulate to high concentrations in trypanosomes. However, the mechanism of action of this class of compounds remains unknown. A long-hy...
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In 1945 Elson showed that certain aromatic diamidines exhibit a marked antifungal activity. More recent studies have found them effective against several pathogenic fungi both in vitro and when used clinically (Curtis and Harrell, 1952; Schoenbach et al., 1952). The diamidines were developed first for use against the trypanosomes and later found useful in certain bacterial infections and neopla...
متن کاملPhenyl substitution of furamidine markedly potentiates its anti-parasitic activity against Trypanosoma cruzi and Leishmania amazonensis.
Furamidine (DB75) and related unfused aromatic diamidines have proven useful for the treatment of parasitic infections. These compounds were primarily developed to combat infections by Pneumocystis carinii and African trypanosomes but they are also active against other parasites. Here we have investigated the in vitro effects of DB75 and its phenyl-substituted analog DB569 on two kinetoplastid ...
متن کاملTrypanothione is the primary target for arsenical drugs against African trypanosomes.
The trypanosomatid metabolite N1,N8-bis-(glutathionyl)spermidine (trypanothione) has been demonstrated to form a stable adduct with the aromatic arsenical drug melarsen oxide [p-(4,6-diamino-s-triazinyl-2-yl)aminophenyl arsenoxide]. The stability constant of the melarsen-trypanothione adduct (Mel T) has been determined to be 1.05 x 10(7) M-1. When bloodstream Trypanosoma brucei are incubated wi...
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تاریخ انتشار 2007