Unravelling the potency of triazole analogues for inhibiting α-synuclein fibrillogenesis and in vitro disaggregation

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dc.contributor.author Maqbool, Mudasir
dc.contributor.author Gadhavi, Joshna
dc.contributor.author Singh, Anju
dc.contributor.author Hivare, Pravin
dc.contributor.author Gupta, Sharad
dc.contributor.author Hoda, Nasimul
dc.coverage.spatial United Kingdom
dc.date.accessioned 2021-02-22T13:54:21Z
dc.date.available 2021-02-22T13:54:21Z
dc.date.issued 2021-01
dc.identifier.citation Maqbool, Mudasir; Gadhavi, Joshna; Singh, Anju; Hivare, Pravin; Gupta, Sharad and Hoda, Nasimul, “Unravelling the potency of triazole analogues for inhibiting α-synuclein fibrillogenesis and in vitro disaggregation”, Organic and Biomolecular Chemistry, DOI: 10.1039/D0OB02226H, vol. 19, no. 7, pp. 1589-1603, Jan. 2021. en_US
dc.identifier.issn 1477-0520
dc.identifier.issn 1477-0539
dc.identifier.uri https://doi.org/10.1039/D0OB02226H
dc.identifier.uri https://repository.iitgn.ac.in/handle/123456789/6305
dc.description.abstract A series of triazole-based compounds was synthesized using a click chemistry approach and evaluated for the inhibition of α-synuclein (α-syn) fibrillogenesis and its disaggregation. Compounds Tr3, Tr7, Tr12, Tr15, and Tr16 exhibited good effect in inhibiting α-syn fibrillogenesis confirmed by Thioflavin-T assay and fluorescence microscopy and α-syn disaggregation confirmed by fluorescence microscopy. Molecular docking was used to understand the plausible mechanism of the test compounds for inhibiting the α-syn fibrillogenesis and to verify the in vitro results. Compounds Tr3, Tr7, Tr12, Tr15 and Tr16 showed good binding interactions with the essential amino acid residues of α-syn. The compounds which were found to be good inhibitors or disaggregators had no toxic effects on the SH-SY5Y cell line. These compounds have the potential to be developed as therapeutic interventions against synucleinopathies including Parkinson's disease and Lewy body dementia.
dc.description.statementofresponsibility by Mudasir Maqbool, Joshna Gadhavi, Anju Singh, Pravin Hivare, Sharad Gupta and Nasimul Hoda
dc.language.iso en_US en_US
dc.publisher Royal Society of Chemistry en_US
dc.subject Triazole en_US
dc.subject Fibrillogenesis en_US
dc.subject Disaggregation en_US
dc.title Unravelling the potency of triazole analogues for inhibiting α-synuclein fibrillogenesis and in vitro disaggregation en_US
dc.type Article en_US
dc.relation.journal Organic and Biomolecular Chemistry


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