Synthesis, characterization and antimalarial evaluation of new β-benzoylstyrene derivatives of acridine

• Main Authors: Sita Prasad Prajapati, Naveen Kumar Kaushik, Mehul Zaveri, Dinesh Mohanakrishanan, Neha Kawathekar, Dinkar Sahal
• Format: Article
• Language: English
• Published: Elsevier 2017-02-01
• Series: Arabian Journal of Chemistry
• Subjects: β-Benzoylstyrene derivatives of acridine; Antimalarial evaluation
• Online Access: http://www.sciencedirect.com/science/article/pii/S187853521200192X

A series of β-benzoylstyrene derivatives of acridine (4a–r) have been synthesized and characterized using IR, 1H NMR and Mass Spectroscopy. All the compounds were screened for intraerythrocytic in vitro antimalarial activity against Chloroquine-sensitive (3D7) & Chloroquine-resistant (Dd2) strains of Plasmodium falciparum using the SYBR Green I fluorescence assay. Cytotoxicity study was performed against the HeLa cell line using the MTT assay. Compounds 4c, 4d, and 4l are most potent with IC50 in the range of 0.30–0.52 μM against the 3D7 strain and 0.15–0.32 μM against the Dd2 strain. The results revealed that antimalarial potency and good resistance indices were not at the cost of safety since the most potent compounds have turned out to have promising therapeutic indices in the range of 80–520.