3-(1,3,4-Thiadiazole-2-yl)quinoline derivatives: Synthesis, characterization and anti-microbial activity

A new series of thiadiazoles and intermediate thiosemicarbazones were synthesized from the chloroquinone molecule, with an aim to explore their effect on in vitro growth of microorganisms causing microbial infection. The chemical structures of the compound were elucidated by elemental analysis, FTIR, 1H and 13C NMR and ESI-MS spectral data. In vitro anti-microbial activity was performed against Staphylococcusaureus, Streptococcuspyogenes, Salmonellatyphimurium, and Escherichiacoli. The MIC was detected using the double dilution method. The results were compared by calculating percent inhibit area/μg of the compounds and the standard “amoxicillin”. The selected compounds were tested for cytotoxic results using MTT assay H9c2 cardiac myoblasts cell line and the results showed that all the compounds offered remarkable >80% viability to a concentration of 200 μg/mL.

Graphical abstract3-(1,3,4-thiadiazol-2-yl)quinoline derivatives were synthesized and screened for anti-microbial activity. Derivatives with higher percent inhibition area than standard drug were screened for toxic effects using H9c2 cardiac myoblasts cell line.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Synthesize of 3-(1,3,4-thiadiazole-2-yl)quinolone, a new series of compounds with low molecular weight. ► Synthesized compounds have two biologically active compounds quinoline and thidiazoles in their basic structural form. ► The intermediate compounds were managed to be stable ones, and were screened for their effect on microorganism growth. ► The intermediate “thiosemicarbazones” and final “thiadiazoles” were screened for gram-negative and positive bacteria and some leads were found. ► Effective compounds were screened for cytotoxic studies, to confirm the toxic nature of the compounds.