IN-VITRO ACTIVITY OF DIOSPYRIN AND DERIVATIVES AGAINST LEISHMANIA-DONOVANI, TRYPANOSOMA-CRUZI AND TRYPANOSOMA-BRUCEI-BRUCEI

Diospyrin and its four synthetic derivatives were tested in vitro agai nst intracellular amastigotes of Leishmania donovani and Trypanosoma c ruzi in macrophages and extracellular Trypansoma brucei brucei bloodst ream form trypomastigotes. Diospyrin was inactive against L. donovani but had ED(50) values of 27 and 50 mu M, respectively, against T. cruz i and T.b. brucei, The dimethyl ether derivative was more active than the parent compound against T. cruzi and T.b. brucei, but the hydroqui nonoid form was the most active antiparasitic agent with ED,, values o f 2.2 and 0.7 mu M, respectively, against L. donovani and T.b. brucei.