Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles

dc.contributor.authorTukulula, Matshawandile
dc.contributor.authorLouw, Stefan
dc.contributor.authorNjoroge, Mathew
dc.contributor.authorChibale, Kelly
dc.date.accessioned2021-10-13T18:32:06Z
dc.date.available2021-10-13T18:32:06Z
dc.date.issued2020-12-15
dc.date.updated2020-12-24T20:36:42Z
dc.description.abstractA second generation of 4-aminoquinoline- and 8-aminoquinoline-based tetrazoles and lactams were synthesized via the Staudinger and Ugi multicomponent reactions. These compounds were subsequently evaluated in vitro for their potential antiplasmodium activity against a multidrug-resistant K1 strain and for their antitrypanosomal activity against a cultured T. b. rhodesiense STIB900 strain. Several of these compounds (4a–g) displayed good antiplasmodium activities (IC50 = 0.20–0.62 µM) that were comparable to the reference drugs, while their antitrypanosomal activity was moderate (200 µM) at pH 7.en_US
dc.identifierdoi: 10.3390/molecules25245941
dc.identifier.apacitationTukulula, M., Louw, S., Njoroge, M., & Chibale, K. (2020). Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles. <i>Molecules</i>, 25(24), http://hdl.handle.net/11427/35234en_ZA
dc.identifier.chicagocitationTukulula, Matshawandile, Stefan Louw, Mathew Njoroge, and Kelly Chibale "Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles." <i>Molecules</i> 25, 24. (2020) http://hdl.handle.net/11427/35234en_ZA
dc.identifier.citationTukulula, M., Louw, S., Njoroge, M. & Chibale, K. 2020. Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles. <i>Molecules.</i> 25(24) http://hdl.handle.net/11427/35234en_ZA
dc.identifier.ris TY - Journal Article AU - Tukulula, Matshawandile AU - Louw, Stefan AU - Njoroge, Mathew AU - Chibale, Kelly AB - A second generation of 4-aminoquinoline- and 8-aminoquinoline-based tetrazoles and lactams were synthesized via the Staudinger and Ugi multicomponent reactions. These compounds were subsequently evaluated in vitro for their potential antiplasmodium activity against a multidrug-resistant K1 strain and for their antitrypanosomal activity against a cultured T. b. rhodesiense STIB900 strain. Several of these compounds (4a–g) displayed good antiplasmodium activities (IC50 = 0.20–0.62 µM) that were comparable to the reference drugs, while their antitrypanosomal activity was moderate (200 µM) at pH 7. DA - 2020-12-15 DB - OpenUCT DP - University of Cape Town IS - 24 J1 - Molecules LK - https://open.uct.ac.za PY - 2020 T1 - Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles TI - Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles UR - http://hdl.handle.net/11427/35234 ER - en_ZA
dc.identifier.urihttps://doi.org/10.3390/molecules25245941
dc.identifier.urihttp://hdl.handle.net/11427/35234
dc.identifier.vancouvercitationTukulula M, Louw S, Njoroge M, Chibale K. Synthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazoles. Molecules. 2020;25(24) http://hdl.handle.net/11427/35234.en_ZA
dc.publisher.departmentDepartment of Chemistryen_US
dc.publisher.facultyFaculty of Scienceen_US
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en_US
dc.sourceMoleculesen_US
dc.source.journalissue24en_US
dc.source.journalvolume25en_US
dc.source.urihttps://www.mdpi.com/journal/molecules
dc.titleSynthesis and In Vitro Antiprotozoan Evaluation of 4-/8-Aminoquinoline-based Lactams and Tetrazolesen_US
dc.typeJournal Articleen_US
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