Synthesis and biological evaluation of pyrazolylnaphthoquinones as new antitrypanosomal and cytotoxic agents

NR SPERANDEO

CHEMBIOCHEM

WILEY-V C H VERLAG GMBH

Lugar: Weinheim; Año: 2003 vol. 4 p. 69 - 69

1439-4227

he importance of American trypanosomiasis (Chagas´ disease) inhuman pathology is widely known. The prognosis of this disease ispoor and the choice of effective medicines limited, thus study ofnew drugs is absolutely necessary. In this work, the activities ofthree new pyrazolylnaphthoquinones, heterocyclic naphthoquinonesbearing 3-aminopyrazole rings, were evaluated on Trypanosomacruzi, the etiological agent of Chagas´ disease. Theseactivities were compared with those of three 5-aminoisoxazoleanalogues. In addition, since these compounds belong to a familyof antiprotozoal and cytotoxic/antitumor agents, the activities ofall six against Plasmodium falciparum, Trypanosoma bruceirhodesiense, and murine L-6 cells were also investigated. In thebiological tests, five of the compounds showed significant in vitrotrypanocidal activities against T. cruzi, with activities similar to thatof benznidazole. Two of the 5-aminoisoxazole analogues alsoshowed good activities, in one case highly selective