Drug Formulation & Bioavailability Congress

Biography

Biography: Azar Tahghighi

Abstract

Parasitic diseases are a major problem in tropical and subtropical regions of the world such as malaria and leishmaniasis. These diseases are the cause of considerable mortality and morbidity annually. No vaccines to prevent infections are available. In the other hand, parasitic drug resistances have restricted the use of available drugs for treatment of malaria and leishmaniasis. Actually, Identification and development of new, cheap, efficient, and safe compounds as drug candidates for the treatment of these diseases are imperative from pharmaceutical point of view. Therefore, a range of creative strategies are required to achieve new lead compounds. The aims of our studies were to synthesis and assess antiparasitic property of 5-(5-nitrohetero aryl-2-yl)-1,3,4-thiadiazoles with different substituents  at the 2-position of  thiadiazole ring. It was notable that the bioresponses and physicochemical properties of the molecules depended on the type of these substituents. In these studies, MLR and ANN models were used for the prediction of the antileishmanial activity of some thiadiazole derivatives. Both of them were successful in predicting the antileishmal activity. Also, molecular modeling and docking studies were conducted based on DNA topoisomerase I as a target enzyme. The results suggested that hydrogen bonding and hydrophobic interactions of ligands with the active site of Leishmania major topoisomerase IB were responsible for their potent antileishmanial activity. Therefore, these results can be used for drug design and development of new and selective leishmania topoisomerase inhibitors.