SYNTHESIS, DOCKING AND EVALUATION OF PYRIMIDINE DERIVATIVES AS ANTI-MALARIAL AGENTS

Abstract

Malaria is endmic disease of tropical and subtropical contries like India, Pakistan, Srilanka, Bangladesh, South Africa etc. There are lot of fatalities and causalities due to malaria every year. There are lot of drugs have been synthesized for controlling this intermittent fever like chloroquine, hydroxychloroquine, pamaquine, primaquine, artimisininine, sulphadoxine, pyrimethamine, dapsone. The pyrimidine derivative synthetic drugs like sulphadoxine and pyramethamine have potential role to treat malaria with fever side effects. The lead molecule is pyrimdine and various groups are attached to this nucleus for optimizing the activity of lead nucleus and its derivative to treat this dangerous disease. The main causative organisms are plasmodium falciparm, plasmodium vivex, plasmodium malariae and ovale that cause malaria in patient and transmitted in blood after bitting of female anopheles mosquito that act as vector for plasmodium species. The docking studies are also performed by software and proper lead compound is identified with docking studies. The synthesis of compounds were carried out in laboratories with  microwave synthesis and newer techniques that are fast and less time consuming of better yield of products. Structure activities relationships are studied and optimum activities are obtained by replacing different functional groups and other groups.