10.1021/acscombsci.5b00044.s002 Ajaz A. Dar Ajaz A. Dar Nagasuresh Enjamuri Nagasuresh Enjamuri Md. Shadab Md. Shadab Nahid Ali Nahid Ali Abu T. Khan Abu T. Khan Synthesis of Unsymmetrical Sulfides and Their Oxidation to Sulfones to Discover Potent Antileishmanial Agents American Chemical Society 2015 presence antimicrobial leishmaniasi compound VL sulfone derivatives Discover Potent Antileishmanial AgentsUnsymmetrical sulfides room temperature 2015-11-09 00:00:00 Journal contribution https://acs.figshare.com/articles/journal_contribution/Synthesis_of_Unsymmetrical_Sulfides_and_Their_Oxidation_to_Sulfones_to_Discover_Potent_Antileishmanial_Agents/2111275 Unsymmetrical sulfides were first synthesized using combinations of a 1,3-dicarbonyl, an aromatic aldehyde and a thiol in the presence of 10 mol % ethanolic piperidine. These sulfides derivatives were subsequently converted into corresponding sulfones via oxidation in the presence of <i>m</i>-chloroperoxybenzoic acid (<i>m</i>-CPBA) at ice-bath to room temperature. The former reaction was achieved at room temperature through one-pot three-component. The later was obtained in good yields using mild reaction conditions with flexibility in choice from a range of substrates. The antimicrobial properties of the newly synthesized sulfone derivatives were investigated against the protozoan parasite, <i>Leishmania donovani</i>, a causative agent of visceral leishmaniasis (VL). Nine sulfone derivatives were found to be efficacious and exhibited significant antimicrobial activity. Further, these compounds were nontoxic on murine peritoneal macrophages thus eliminating potential cytoxicity in the host cells. These compounds may be indicated as potential leads in the treatment of visceral leishmaniasis.