Anilino-(2-Bromophenyl) Acetonitrile and Their Analogues as Orally Effective Antileishmanial Agents

概要

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Visceral leishmaniasis (VL) or kala-azar is a worldwide disseminated intracellular infection caused by the hemoflagellate protozoan parasites Leishmania donovani. Chemotherapeutic scenario presents a deplorable picture and demands an urgent search for a new and safe anti-VL drugs, preferably active by oral route. In search of new antileishmanial agents, a total of 16 compounds belonging to the anilino-(substituted pnenyl)-acetonitrile class were tested in-vitro in promastigote/macrophase-amastigote systems and in-vivo in L. donovani/hamster model for their antileishmanial activity.. Compound 3, anilino-(2-bromophenyl)-acetonitrile, exhibited most promising activity both in-vitro at a concentration of 100μg/ml (82.33% and 94.36% in promastigote and macrophase-amastigote systems respectively) and in-vivo at a dose of 50 mg/kg for 5 days (82.12% and 80% by i.p. and p.o. routes respectively), hence this compound was investigated in detail. To maximize its bioavailability, dissolution profile, absorption, the compound was also tested in-vivo as its soluble form. But no enhancement in activity was observed. From the results of different parameters for example ED_<50> and LD_<50> etc. compound 3 appears to be a potent orally effective compound which could further be investigated to establish its potential as a candidate molecule of antileishmanial therapy.
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