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.