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Synthesis of Unsymmetrical Sulfides and Their Oxidation to Sulfones to Discover Potent Antileishmanial Agents

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Title Synthesis of Unsymmetrical Sulfides and Their Oxidation to Sulfones to Discover Potent Antileishmanial Agents
 
Creator Dar, Ajaz A
Enjamuri, Nagasuresh
Shadab, Md. Shadab
Ali, Nahid
Khan, Abu T
 
Subject Infectious Diseases and Immunology
 
Description 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 m-chloroperoxybenzoic acid (m-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, Leishmania donovani, 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
 
Date 2015
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://www.eprints.iicb.res.in/2455/1/ACS_COMBINATORIAL_SCIENCE__Vol._17____(11)___671%2D681;_2015.pdf
Dar, Ajaz A and Enjamuri, Nagasuresh and Shadab, Md. Shadab and Ali, Nahid and Khan, Abu T (2015) Synthesis of Unsymmetrical Sulfides and Their Oxidation to Sulfones to Discover Potent Antileishmanial Agents. ACS Combinatorial Science, 17 (11). pp. 671-681.
 
Relation http://dx.doi.org/10.1021/acscombsci.5b00044
http://www.eprints.iicb.res.in/2455/