Trypanocidal agents

Isatin serves as a substrate for the biosynthesis of violacein, a trypanocide agent, by Chromobacterium violaceum. ... 

Trusopi. Sec Dor/olamide Trypanocidal agents. 668 Trypanosomiasis, 260 Trypsin cry.slallized. 8.38. K39l Tryptophan... 

Antineoplastic agent Enzyme inhibitors Trypanocidal agent... 

A number of drugs, which are known to bind with tubulin and inhibit its polymerisation to microtubules, have been evaluated in protozoal chemotherapy. The most notable are the alkaloids maytansine, ansamitocin P3, vinblastine and vin-cristin, which have been shown to be potent inhibitors of tubulin polymerisation in T. brucei. However, these are too toxic to be considered as useful trypanocidal agents [2]. 

Loiseau PM, Lubert P, Wolf JG (2000) Contribution of dithiol ligands to In vitro and In vivo trypanocidal activities of dithiaarsanes and investigation of ligand exchange in an aqueous solution. Antimicrob Agents Chemother 44 2954—2961... 

Extracts of baobab root are trypanocidal to either Trypanosoma brucei brucei and T. congolense. T. brucei brucei and T. congolense are unicellular parasites transmitted by the bites of tsetse fly and is the causative agent of sleeping sickness in humans and related diseases in animals (27). 

Garcinia intermedia Pittier Hammei (leaves) Biflavones. Podocarpusflavone A (6) amentoflavone (1). Trypanocidal activity against epimastigotes of Trypanosoma cruzi, the etiologic agent of Chagas disease. Abe et al., 2004[170]. 

In African trypanosomes this enzyme also cleaves 5 -halo- and ethylthioribose derivatives of MTA to produce adenine plus the resulting ribose analog (74). The latter would normally be recycled to methionine (5). These agents are trypanocidal and their effects can be reversed with methionine or ketomethylthiobutyrate, an intermediate in the conversion of methylthioribose into methionine (74). 

Bacchi, C. J., Sufrin, J., Nathan, H. C. et al. (1991) 5 -Alkyl-substituted analogs of 5 -methyl-thioadenosine as trypanocides. Antimicrob. Agents Chemother. 35 1315-1320. 

Because parasites are dependent on the host cell for nutrients and essential components, the arguments mentioned previously for alteration of the optimal metal concentration and its application to antibacterial and antiviral therapy are equally valid in the case of parasites. The sequestration of zinc and subsequent biochemical effects may present an example of this and the behaviour is somewhat reminiscent of the early and classic demonstration of the mode of action of 8-hydroxyquinoline (oxine). This reagent is also trypanocidal and, as with bacterial systems, cobalt protects against the lethal action [88]. The mode of action of oxine is presumably the same as for bacteria (see Chapter 9). Other chelating agents studied in... 

METAL COMPLEXES WITH TRYPANOCIDAL DRUGS. DUAL-FUNCTION AGENTS... 

Sufrin JR, Spiess AJ, Marasco CJ Jr, Rattendi D, Bacchi CJ (2008) Novel trypanocidal analogs of 5 -(methylthio)-adenosine. Antimicrob Agents Chemother 52 211-219... 

M.L. Stewart, G.J. Bueno, A. Baliani, B. Klenke, R. Brun, J.M. Brock, I.H. Gilbert, M.P. Barrett, Trypanocidal activity of melamine-based nitro-heterocydes, Antimicrob. Agents Chemother. 48 (2004) 1733-1738. 

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