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Research and development for novel antimicrobial drugs having different mode of action has become an urgent task for scientific community because of escalating resistance towards currently used antibiotics in clinical practice. The menace of microbial resistance may be dealt with novel antimicrobial drugs of natural and synthetic origin as per the recent most literature. This communication is a coherent endeavor to summarize the potent antimicrobial profiles of various heterocyclic derivatives for drug design and development of promising and advanced antimicrobial drugs in search of providing better treatment to the patients globally.