Identifying the Issue
Malarial parasites are becoming resistant to presently used drugs, for this reason, there is a need for new and better antimalarial drugs.
Objective of the Research
To semi-synthesize isoandrographolide acetals from the natural product andrographolide and study their antimalarial potency.
Who should read this?
Faculty, research scholars, and students of Medicinal and Organic chemistry.
Solution
Isoandrographolide and its nineteen acetals were synthesized and characterized using 1H-NMR, 13C-NMR, mass spectrometry, IR, and UV spectroscopy. Out of these fifteen isoandrographolide acetals are novel. The compound (3,19)-4-Methoxy-benzylidene-isoandrographolide was characterized using single-crystal X-ray diffraction also. All the compounds were tested for their anti-plasmodial potencies (IC50) against the chloroquine-sensitive Pf3D7 and chloroquine-resistant PfINDO strains. Potent compounds were further tested for their cytotoxicity (CC50) against mammalian cells. The activity of the compounds is influenced by various factors like the type of substituent, its position, and also its bulkiness. Thus, from this study it can be concluded that acetals of isoandrographolide can be explored as potential anti-plasmodial leads.
Key Features and Benefits
Impact
Potential as leads in the development of antimalarial drugs
Team
Title of paper: Synthesis and Anti‑Plasmodial Activity f Isoandrographolide Acetals
Read Paper Here: https://doi.org/10.1007/s11696-023-02684-9
