7-Chloroquinoline Sulphonamide Derivatives: Synthesis, Characterization, Biological and Drug-likeness Evaluation

Abstract

New quinoline derivatives incorporating sulphonamide moieties have been synthesized from 4,7-dichloroquinoline and characterized using 1HNMR, 13CNMR and FTIR techniques. The compounds were screened for their in-vitro antibacterial activity against Gram-positive (Staphylococcus aureus,Bacillus subtilis) and Gram-negative (Escherichia coli, Klebsiella pneumoniae) bacteria species. The antibacterial activities were determined using standard methods.

Among the tested compounds, it was found that compound 2 had the most potent antibacterial activity against all the tested strains except B. subtilis, but lower antibacterial activity than ciprofloxacin. The compounds indicated strong antifungal activity against Penicillium simplicissimum and Aspergillus niger with compound 6 revealing the highest activity with the inhibition zone diameter (IZD) of 28 mm. Compounds 2, 3, 4 and 6 showed more potent antifungal inhibitory activities against the two tested fungal species than fluconazole. The ADME (Adsorption, Distribution, Metabolism and Excretion) prediction indicated that the compounds possessed desirable drug-like properties for good bioavailability