This book narrates methods to synthesize some novel antimicrobial chemical entities (NCEs). It also depicts a hybrid approach for combining two or more frameworks in a single scaffold to enhance the predicted activity. This study also discusses the characterization of synthesized molecules by the latest spectroscopic techniques like 1H and 13C NMR, IR, and mass. In this study, we have identified some molecules which are highly active as antimicrobial agents. Also in it, we have discussed the cause of biological activity. These molecules may be modified as per the requirement to be a drug candidate.