Detail of "187949-02-6"

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Activity of the new triazole derivative albaconazole against Trypanosoma (Schizotrypanum) cruzi in dog hosts

Activity of the new triazole derivative albaconazole against Trypanosoma (Schizotrypanum) cruzi in dog hosts. da Matta Guedes, Paulo Marcos; Urbina, Julio A.; de Lana, Marta; Afonso, Luis C. C.; Veloso, Vanja M.; Tafuri, Washington L.; Machado-Coelho, George L. L.; Chiari, Egler; Bahia, Maria Terezinha ( Departmento de Ciencias Biologicas, Universidade Federal de Ouro Preto, Ouro Preto, Brazil). Antimicrobial Agents and Chemotherapy, 48(11), 4286-4292 (English) 2004 American Society for Microbiology. CODEN: AMACCQ. ISSN: 0066-4804. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Albaconazole is an exptl. triazole deriv. with potent and broad-spectrum antifungal activity and a remarkably long half-life in dogs, monkeys, and humans. In the present work, the authors investigated the in vivo activity of this compd. against two strains of the protozoan parasite Trypanosoma (Schizotrypanum) cruzi, the causative agent of Chagas' disease, using dogs as hosts. The T. cruzi strains used in the study were previously characterized (murine model) as susceptible (strain Berenice-78) and partially resistant (strain Y) to the drugs currently in clin. use, nifurtimox and benznidazole. Our results demonstrated that albaconazole is very effective in suppressing the proliferation of the parasite and preventing the death of infected animals. Furthermore, the parasitol., PCR, serol., and proliferative assay results indicated parasitol. cure indexes of 25 and 100% among animals inoculated with T. cruzi strain Y when they were treated with albaconazole at 1.5 mg/kg of body wt./day for 60 and 90 days, resp. On the other hand, although albaconazole given at 1.5 mg/kg/day was very effective in suppressing the proliferation of the parasite in animals infected with the Berenice-78 T. cruzi strain, no parasitol. cure was obsd. among them, even when a longer treatment period (150 doses) was used. In conclusion, our results demonstrate that albaconazole has trypanocidal activity in vivo and is capable of inducing radical parasitol. cure, although natural resistance to this compd. was also indicated. Furthermore, the compd. can be used in long-term treatment schemes (60 to 150 days) with minimal toxicity and thus represents a potentially useful candidate for the treatment of human Chagas' disease.Except for chemicals metioned above, 187949-02-6 and 22994-85-0 are also used. .