One-compound-two-pharmacophores: design, synthesis and antimalarial activities of chloroquinoline-cassiarin

Thobias Kalenga, Monica Ndoile, Quintino Mgani


This 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 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.

Key Words: Chloroquinoline-cassiarin, Barakol, Antimalarial, Cassiarin, Cassia siamea

Full Text:



  • There are currently no refbacks.