DESIGN AND SYNTHESIS OF TRIAZINE DERIVATIVES AS ANTIMALARIAL AGENTS

Reshma P. Pore* and Supriya S. Mahajan

ABSTRACT

Malaria imposes great socio-economic burden on humanity, and with six other diseases (diarrhoea, HIV/AIDS, tuberculosis, measles, hepatitis B, and pneumonia), accounts for 85% of global infectious disease burden. Drug resistance in malarial parasite has become one of the most important problems in the disease control in recent years. Resistance has been reported in almost all the antimalarial drugs, including artemisinin. Considering this aspect, development of new drugs is of primary importance. The computer aided drug designing (CADD) is an advanced, novel and convenient technique. With the help of CADD, one can design drug molecules and also predict the drug-receptor binding. In the current study, a series of triazine derivatives were designed as inhibitors of wild PfDHFR and quadruple mutant PfDHFR enzyme. Compounds with good G-score were synthesized on the laboratory scale. The compounds would be evaluated for antimalarial activity, in vivo against Plasmodium berghei and in vitro against chloroquine resistant W2 strain of Plasmodium falciparum.

Keywords: Malaria, drug resistance, computer aided drug designing, Plasmodium falciparum, triazines.