ONE-COMPOUND-TWO-PHARMACOPHORES: DESIGN, SYNTHESIS AND ANTIMALARIAL ACTIVITIES OF CHLOROQUINOLINE-CASSIARIN

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dc.creatorKalenga, Thobias
dc.creatorNdoile, Monica
dc.creatorMgani, Quintino
dc.date2018-09-10T11:36:59Z
dc.date2018-09-10T11:36:59Z
dc.date2018
dc.date.accessioned2021-05-03T13:19:55Z
dc.date.available2021-05-03T13:19:55Z
dc.descriptionThis paper describes the design and synthesis of a potential antimalarial compound, chloroquinoline-cassiarin (6) using 4,7-dichloroquinoline and the natural product barakol (1) extracted from the leaves of Cassia siamea as starting materials. In this paper a one compound-two-pharmacophores concept is introduced in which coupling of two known pharmacophores into one has been described. The concept is not only useful to organic synthesis but also to drug development researches. The synthesized compound 6 exhibited potent in vitro antimalarial activity at IC50 = 0.51 μM, and low toxicity where at 20 μM, 80% viability of HeLa cells was observed.
dc.identifierKalenga, T., Ndoile, M., & Mgani, Q. (2018). One-compound-two-pharmacophores: design, synthesis and antimalarial activities of chloroquinoline-cassiarin. Tanzania Journal of Science, 44(2), 154-161.
dc.identifierhttp://hdl.handle.net/20.500.11810/4871
dc.identifier.urihttp://hdl.handle.net/20.500.11810/4871
dc.subjectChloroquinoline-cassiarin
dc.subjectBarakol
dc.subjectAntimalarial
dc.subjectCassiarin
dc.subjectCassia siamea
dc.titleONE-COMPOUND-TWO-PHARMACOPHORES: DESIGN, SYNTHESIS AND ANTIMALARIAL ACTIVITIES OF CHLOROQUINOLINE-CASSIARIN
dc.typeJournal Article, Peer Reviewed

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