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October 21, 2025Russian Chemical Reviews3 citations

Recent advances in the synthesis of pharmacologically active 1,2,3-, 1,2,4-, and 1,2,5-oxadiazole-based lead compounds

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ISI. A. StebletsovaALAlexander А. LarinЛФЛеонид Л. Ферштат

Key Points

  • Oxadiazole derivatives demonstrate diverse pharmacological activity, including antimicrobial and antiinflammatory effects.
  • The review covers advancements in synthesis techniques over the past decade, showcasing 173 references.
  • Key structure–property relationships for oxadiazole derivatives are outlined, offering guidelines for pharmaceutical design.
  • Hybrid molecules featuring oxadiazoles show promising potential for developing new therapeutic agents.

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.

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Stebletsova et al. (2025) studied this question.

synapsesocial.com/papers/68f74e597f21f73e19e5b551https://doi.org/10.59761/rcr5185
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