Abstract: Nitrogen heterocycles hold leading positions in the field of medicinal chemistry and targeted search for next-generation pharmaceuticals. Among the enormous set of available heterocyclic structures, oxadiazole derivatives attract attention of scientists due to a wide range of pharmacological activity, including antimicrobial, antiinflammatory, antiproliferative, and other types of activity. This review summarizes the achievements in the field of synthesis and biological activity of oxadiazole derivatives over the past 10 years. Methods for the synthesis of various therapeutic agents based on 1,2,3- 1,2,4- and 1,2,5-oxadiazoles are considered, and new approaches to the fabrication of hybrid molecules (hybrids) consisting of two or more pharmacophore moieties are systematized. The review provides the first comprehensive consideration of the key structure–property relationships for each type of oxadiazole derivatives, which can serve as guidelines for specialists in various fields who develop strategies for the design of new pharmaceuticals. The bibliography includes 173 references.

Cite: Stebletsova I.A. , Larin A.A. , Fershtat L.L.
Recent advances in the synthesis of pharmacologically active 1,2,3-, 1,2,4-, and 1,2,5-oxadiazole-based lead compounds
Russian Chemical Reviews. 2025. V.94. N10. RCR5185 . DOI: 10.59761/rcr5185 WOS Scopus OpenAlex

Identifiers:

Web of science:	WOS:001611005800003
Scopus:	2-s2.0-105027471133
OpenAlex:	W4415369082

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