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Updated: Jul 1, 2025

High Throughput, Real-time, Dual-readout Testing of Intracellular Antimicrobial Activity and Eukaryotic Cell Cytotoxicity
Published on: November 16, 2016
Exploring the antimicrobial and cytotoxic potential of novel chloroquine analogues
Shamsul Islam1, Sohail A Shahzad2, Tariq Ismail1
1Department of Pharmacy, COMSATS University Islamabad, Abbottabad Campus, Abbottabad, 22060, Pakistan.
Abstract:
Aim: To synthesize novel chloroquine analogues and evaluate them for antimicrobial and cytotoxic potential. Methods: Novel analogues were synthesized from chloroquine by nucleophilic substitution reaction at the 4-amino position. Results: Analogue CS1 showed maximum antimicrobial potential (30.3 ± 0.15 mm zone) against Pseudomonas aeruginosa and produced a 19.2 ± 0.21 mm zone against Candida albicans, while CS0 produced no zone at the same concentration. Analogue CS9 has excellent cytotoxic potential (HeLa cell line), showing 100% inhibition (IC50 = 8.9 ± 1.2 μg/ml), compared with CS0 (61.9% inhibition at 30 μg/ml). Conclusion: These synthesized chloroquine analogues have excellent activity against different microbial strains and cervical cancer cell lines (HeLa) compared with their parent molecule.

