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This book describes the synthesis of some novel s-triazinyl thiourea congeners endowed with various aromatic amine as well as piperazine motifs via an efficient and sustainable copper catalyzed coupling. Development of optimized method for the synthesis of many heterocyclic moieties is still a challenge. We have developed an efficient technique to synthesize thiourea derivatives using Copper as catalyst in order to prepare effective antimicrobial agents. All the newly prepared scaffolds were fully characterized and evaluated for their in vitro antibacterial, antifungal as well as anti-TB activity.