Discovery of 3,3'-diindolylmethanes as potent antileishmanial agents
IR@CIMFR: CSIR-Central Institute of Mining and Fuel Research, Dhanbad
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| Title |
Discovery of 3,3'-diindolylmethanes as potent antileishmanial agents
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| Creator |
Maity, Sudip
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| Subject |
Coal Characterisation
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| Description |
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
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| Publisher |
Elsevier
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| Date |
2013-05
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| Type |
Article
PeerReviewed |
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| Format |
application/pdf
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| Identifier |
http://cimfr.csircentral.net/1732/1/Maity%20s..pdf
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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| Relation |
http://dx.doi.org/10.1016/j.ejmech.2013.02.024
http://cimfr.csircentral.net/1732/ |
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