SYNTHESIS AND BIOLOGICAL EVALUATION OF 4-CHLORO-3,5-DINITROBENZOTRIFLUORIDE ANALOGS AS ANTILEISHMANIAL AGENTS

Desnitro analogues of 4-chloro-3,5-dinitrobenzotrifluoride (chloralin) (2), an in vitro microtubule inhibitor of several Leishmania species, have been synthesized from 2-halo-5-(trifluoromethyl)benzenesulfonyl chlorides 4 and 5. The analogues exhibited moderate to excellent activ ity when tested against Leishmania donovani amastigotes in vitro. Two representative compounds, 7f and 8, were tested against the Khartoum s train of L. donovani in a hamster model using chloralin (2) and Glucan time (one of the current therapeutics of choice in the treatment of Le ishmania) as standards, the results of which will be discussed herein.