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

dc.contributor.authorKalenga, Thobias
dc.contributor.authorNdoile, Monica
dc.contributor.authorMgani, Quintino
dc.date.accessioned2018-09-10T11:36:59Z
dc.date.available2018-09-10T11:36:59Z
dc.date.issued2018
dc.description.abstractThis 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.en_US
dc.identifier.citationKalenga, 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.en_US
dc.identifier.urihttp://hdl.handle.net/20.500.11810/4871
dc.subjectChloroquinoline-cassiarinen_US
dc.subjectBarakolen_US
dc.subjectAntimalarialen_US
dc.subjectCassiarinen_US
dc.subjectCassia siameaen_US
dc.titleONE-COMPOUND-TWO-PHARMACOPHORES: DESIGN, SYNTHESIS AND ANTIMALARIAL ACTIVITIES OF CHLOROQUINOLINE-CASSIARINen_US
dc.typeJournal Article, Peer Revieweden_US
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