Microbial infections remain a worldwide leading cause of death, despite the evolution of a large number of new antibiotics every year. Currently, several bacteria have developed resistance against antibiotics drugs which remain a major issue in antibiotics drug discovery. This review provides detailed information about antimicrobial and antifungal agent synthesis belonging to the pyrazoles scaffold. We reassemble the results obtained from several studies to characterize the importance of heteroatom nuclei in many synthetic products. Additionally, several compounds based on pyrazole derivatives such as benzimidazole, benzothiazole, indole, acridine, oxadiazole, imidazole, isoxazole, pyrazole, triazole, quinoline and quinazoline including other pyrazole containing drugs such as pyridazine, pyridine and pyrimidine are highlighted. Furthermore, you will find in this review 134 best promise structures collected from recent studies, relating the pyrazoles structures to the relevant biological activities, in particular, antimicrobial and antifungal one.