Maity, Sudip (2013) Discovery of 3,3'-diindolylmethanes as potent antileishmanial agents. European Journal of Medicinal Chemistry, 63. pp. 435-443. ISSN 0223-5234

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An efficient protocol for synthesis of 3,3′-diindolylmethanes using recyclable Fe-pillared interlayered clay (Fe-PILC) catalyst under aqueous medium has been developed. All synthesized 3,3′-diindolylmethanes showed promising antileishmanial activity againstLeishmania donovani promastigotes as well as axenic amastigotes. Structure–activity relationship analysis revealed that nitroaryl substituted diindolylmethanes showed potent antileishmanial activity. The 4-nitrophenyl linked 3,3′-diindolylmethane 8g was found to be the most potent antileishmanial analog showing IC50 values of 7.88 and 8.37 μM against both L. donovani promastigotes and amastigotes, respectively. Further, a pharmacophore based QSAR model was established to understand the crucial molecular features of 3,3′-diindolylmethanes essential for potent antileishmanial activity. These compounds also exhibited promising antifungal activity against Cryptococcus neoformans, wherein fluorophenyl substituted 3,3′-diindolylmethanes were found to be most potent antifungal agents. Developed synthetic protocol will be useful for economical and eco-friendly synthesis of potent antileishmanial and antifungal 3,3′-diindolylmethane class of compounds

Item Type: Article
Subjects: Coal Characterisation
Depositing User: Mr. B. R. Panduranga
Date Deposited: 06 May 2017 06:34
Last Modified: 06 May 2017 06:34

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