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dc.contributor.authorNandikolla, Adinarayana
dc.contributor.authorSrinivasarao, Singireddi
dc.contributor.authorKaran Kumar, Banoth
dc.contributor.authorMurugesan, Sankaranarayanan
dc.contributor.authorAggarwal, Himanshu
dc.contributor.authorMajor, Louise L.
dc.contributor.authorSmith, Terry K.
dc.contributor.authorChandra Sekhar, Kondapalli Venkata Gowri
dc.date.accessioned2020-11-13T15:30:06Z
dc.date.available2020-11-13T15:30:06Z
dc.date.issued2020-10-19
dc.identifier.citationNandikolla , A , Srinivasarao , S , Karan Kumar , B , Murugesan , S , Aggarwal , H , Major , L L , Smith , T K & Chandra Sekhar , K V G 2020 , ' Synthesis, study of antileishmanial and antitrypanosomal activity of imidazo pyridine fused triazole analogues ' , RSC Advances , vol. 10 , no. 63 , pp. 38328-38343 . https://doi.org/10.1039/d0ra07881fen
dc.identifier.issn2046-2069
dc.identifier.otherPURE: 271203067
dc.identifier.otherPURE UUID: c34205b0-53f4-4905-9904-459038efed78
dc.identifier.otherScopus: 85094905798
dc.identifier.otherORCID: /0000-0001-5287-4488/work/83481380
dc.identifier.otherWOS: 000586355800021
dc.identifier.urihttp://hdl.handle.net/10023/20969
dc.descriptionKVGCS and SM thank DBT, New Delhi [BT/IN/Spain/39/SMl2017-18] for providing financial support. The financial assistance provided by DIST FIST grant (SR/FST/CSI-240/2012), New Delhi is gratefully acknowledged. SS thanks CSIR for providing SRF fellowship.en
dc.description.abstractFour groups, thirty-five compounds in total, of novel 1,2,3-triazole analogues of imidazo-[1,2-a]-pyridine-3-carboxamides were designed and synthesized using substituted pyridine, propargyl bromide, 2-azidoethyl 4-methyl benzenesulfonate and substituted acetylenes. These compounds were characterized using 1H NMR, 13C NMR, LCMS and elemental analyses and a crystal structure was obtained for one of the significantly active compounds, 8f. All the synthesized and characterized compounds were screened in vitro for antileishmanial and antitrypanosomal activity against Leishmania major and Trypanosoma brucei parasites, respectively. Among the tested analogues, fivecompounds (8d, 8f, 8j, 10b and 10d) exhibited significant antileishmanial activity while three compounds (10b, 11a and 11b) showed substantial activity against T. brucei parasite. In silico ADME prediction studies depicted that the essential compounds obeyed Lipinski's rule of five. The predicted in silico toxicity profile suggested that the tested compounds would be non-toxic, which was confirmed experimentally by the lack of cytotoxicity against HeLa cells. Finally, a molecular docking study was also performed, for 10d the most active antileishmanial compound, to study its putative binding pattern at the active site of the selected leishmanial trypanothione reductase target.
dc.format.extent16
dc.language.isoeng
dc.relation.ispartofRSC Advancesen
dc.rightsCopyright © 2020 The Author(s). Open Access Article. This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.en
dc.subjectBIOLOGICAL EVALUATIONen
dc.subjectMEDICINAL ATTRIBUTESen
dc.subject1,2,3-TRIAZOLESen
dc.subjectDERIVATIVESen
dc.subjectACIDen
dc.subjectINHIBITORSen
dc.subjectQD Chemistryen
dc.subjectRM Therapeutics. Pharmacologyen
dc.subjectChemical Engineering(all)en
dc.subjectChemistry(all)en
dc.subjectDASen
dc.subject.lccQDen
dc.subject.lccRMen
dc.titleSynthesis, study of antileishmanial and antitrypanosomal activity of imidazo pyridine fused triazole analoguesen
dc.typeJournal articleen
dc.description.versionPublisher PDFen
dc.contributor.institutionUniversity of St Andrews.School of Biologyen
dc.contributor.institutionUniversity of St Andrews.Biomedical Sciences Research Complexen
dc.identifier.doihttps://doi.org/10.1039/d0ra07881f
dc.description.statusPeer revieweden


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