Abstract
A rational approach was used to synthesize a new set of 15 1H-1,2,4-triazol-3-yl benzenesulfonamide derivatives with the aim of developing new antimalarial lead compounds. These derivatives were prepared in yields between 50% and 62%, and their structures were elucidated using IR, 1H-, 13C-, 19F-NMR, MS and elemental analysis. A docking study based on sulfonamides previously used against malaria identified trifluoromethyl-substituted derivatives to be the best lead compounds for new antimalarial drug development.
Highlights
Malaria is a deadly mosquito-borne disease that afflicts as many as half a billion people; about250 million malaria cases and nearly one million associated deaths have been reported in 106 countries across Africa, Asia and Latin America [1]
The nucleophilic substitution reactions between 3-amino-1H-1,2,4-triazoles 5–7 and sulfonyl chloride derivatives 8–12 were performed under magnetic stirring at room temperature in acetonitrile or DMF, for derivatives 5–6 and 7, respectively, to prepare 1H-1,2,4-triazol-3-yl benzenesulfonamide derivatives 13–27 in moderate yields (50%–62%)
In the 1H-Nuclear Magnetic Resonance (NMR) spectra, the signals of the respective protons of the synthesized compounds were verified on the basis of their chemical shifts, multiplicities and coupling constants
Summary
Malaria is a deadly mosquito-borne disease that afflicts as many as half a billion people; about250 million malaria cases and nearly one million associated deaths have been reported in 106 countries across Africa, Asia and Latin America [1]. Drug resistance, documented in Plasmodium falciparum, P. malariae and P. vivax malaria species, has been one of the main obstacles in the fight against malaria. Increasing resistance to antimalarial drugs has a number of implications for the eradication of malaria. Inappropriate use of antimalarial drugs and the use of monotherapies or substandard and counterfeit medicines are suggested to be the main contributors to widespread resistance in malaria parasites [2]. Chemotherapeutic treatment of malaria can involve a number of compounds: quinine, chloroquine, mefloquine, primaquine, amodiaquine, proguanil, pyrimethamine, sulfadoxine, artemisinin, halofantrine, pyronaridine, piperaquine, and artemisinin derivatives, such as artemether, artesunate and dihydroartemisinin. In the absence of an effective vaccine, and given the decreased efficiency of classical medications against chloroquine-resistant strains, new antimalarial drugs that are efficient, safe and synthetically economical are needed [3,4]
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