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 ompounds possessed desirable drug-like  properties for good bioavailability