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This book describes the synthesis of some new quinolinyl thiourea scaffolds endowed with ether/thioether linkage via an efficient ligand free copper catalyzed C-O/C-S coupling under air atmospheric condition; make the presented methodology extremely valuable from economic and environmental point of view. All the newly synthesized quinoline derivatives were well characterized and evaluated for their in vitro antibacterial, antifungal as well as anti-TB activity.