Drug repositioning involves the investigation of existing drugs and their derivatives for new therapeutic purposes. Due to the widespread biological importance of quinoline, new series of novel quinolines (modified amodiaquine) analogues were synthesized. ¹H NMR, ¹³C NMR and FT-IR were used for characterization. In antibacterial screening, analogue AA1 showed a 12 ± 1.1 mm and 14 ± 0.5mm zone of inhibition against S. aureus and P. aeruginosa respectively. Our analogues (AA1 and AA22) showed a 13 mm zone against E. Coli and AA2 has a 12 ± 0.5 mm zone against Bacillus subtilis. Excellent activity against fungal strains i.e. C. albicans (13 ± 0.5mm) zone was shown by analogue AA1 and AA2. Analogue AA2 showed 100% inhibition with IC₅₀ 11.1 ± 1.1 μg/ml against the HeLa cell line and binding energy against 1PFK (-6.123772 kcal/mol) and 1TUP (-6.512972 kcal/mol) in the docking study. New analogues have excellent activity against different microbial strains and Hela cell-line as compared to their parent molecule.

Keywords: Quinoline analogues, inhibitory concentration, MTT assay, amodiaquine.