Abstract:
A series of 2,4,6-trisubstituted pyrimidines and 1,3,5-triazines have been synthesized and screened for their in vitro and in vivo antileishmanial activity against L. donovani. Among all, 14 compounds have shown promising inhibition of 80-100% at 10 µg/ml against promastigotes and IC50 in the range of 0.89-9.68 µg/ml against amastigotes. Three compounds 13, 32 and 33 with good selectivity index (S.I) were screened for their in vivo activity in golden hamsters (Mesocricetus auretus) infected with MHOM/IN/80/Dd8 strain of L. donovani and have shown moderate in vivo inhibition of 48-56 % at a dose of 50 mg/Kgx5, I.P route for 5 days.
