Scientific publications of recent years clearly demonstrate the prospects of finding new molecules among 1,2,4-triazole derivatives. The whole series of drugs, which are 1,2,4-triazole derivatives (fluconazole, ribavirin, avesstym, tryfuzol and others), are included into the practice of modern medicine, pharmacy and veterinary. Aim. We have studied and analyzed the available scientific sources over the past five years in order to systematize the available literature of recent years about research regarding heterocyclization reactions of 3-thio- and 3-thio-4-amino derivatives of 1,2,4-triazole. During this studying we used methods of observation, systematization and content analysis. Results. It has been found that a comprehensive approach to an objective analysis of scientific literature confirms the possibility of limitless and very attractive scientific research of new molecules that are formed during heterocyclization of 3-thio- and 3-thio-4-amino derivatives of 1,2,4-triazole. Conclusions. Our research shows the promising future for the new original drugs based on 3-thio- and 3-thio-4-amino substituted of 1,2,4-triazole.