Original articleSynthesis and antileishmanial activity of novel 2,4,6-trisubstituted pyrimidines and 1,3,5-triazines

Add time:09/25/2019    Source:sciencedirect.com

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 Leishmania 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 auratus) 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/kg × 5, i.p. route for 5 days.

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