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Background: Thioureas are widely used as intermediates in organic synthesis, and they are commonly used in several classes of heterocycles. Objective: There has been an escalating interest in the development of heterocycles employing thioureas as building blocks. Furthermore, thioureas can be utilized as a reagent in a synthesis of a large number of therapeutic agents. In addition, substituted thioureas have recently gained much interest in the preparation of a wide variety of biologically active compounds. Conclusion: This review highlights the status of thiourea scaffolds in the drug development and heterocyclic synthesis described in the literature mainly since 2010.