Synthesis of some novel and potent anti-plasmodial aminoalkyl chalcone derivatives

Abstract

Malaria remains to be a health and an economic burden to many people living in Sub-Sahara and Africa. According to World health Organization (WHO) in 2017, 219 million cases of malaria worldwide were documented. Its increase by 2 million from the year 2016 resulted in 435 thousand deaths every day among 1190 deaths of young children more than cases 5 per day have been reported. Among the different species of plasmodium parasite, Plasmodium falciparum is mainly responsible for causing malaria in Africa whereas Plasmodium vivax is the most prevalent in countries outside Africa. Africa suffers from malaria a lot. Almost half of the world’s population is at risk of contracting malaria and approximately 90% of the death cases of Malaria in the world appear from Africa. In our research group in past, we have established that chalcones with an aminoalkyl moiety on one of the aromatic rings have promising in vitro antimalarial activity. We successively enhanced the bioavailability from 3% to 25% in mice model with the derivatization of the potential leads with the help of substitutions of the function groups at 4-position from-F to-CF3.