SYNTHESIS, ANTIMALARIAL ACTIVITY AND QSAR STUDIES OF CHALCONES,N-BENZYLIDENESULFONAMIDES AND CHALCONESULFONAMIDES

Malaria remains the major cause of human morbidity and mortality worldwide. Malaria, caused byPlasmodium species, is potentially life threatening, increasing in prevalence and becoming evenmore resistant to in-use drugs. In this article, synthesis of compounds from the series of chalcones,benzylidenesulfonamides and chalconesulfonamides, by the conventional and microwave-irradiationmethods is discussed. The microwave-irradiation method was convenient, rapid and high yielding ascompared to the conventional method of synthesis. The acute oral toxicity studies indicated that all thecompounds were safe for administration up to 2000 mg/kg body weight of a mouse. The compoundswere screened for their antimalarial activity. Two chalcones, five benzylidenesulfonamides and threechalconesulfonamides showed antimalarial activity equivalent to chloroquine. Benzylidenesulfonamidesshowed better antimalarial activity compared to the compounds from the other two series.Chalconesulfonamides showed better antimalarial activity than chalcones. The QSAR studies werecarried out by correlating antimalarial activity of all the compounds with their physicochemical descriptors.Validation of the best QSAR model was carried out using the training set and the test set method. Thesestudies provided guidance for the development of novel antimalarials from these series.