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Novel 1,2,4-Oxadiazole Derivatives in Drug Discovery

1
Department of Organic Chemistry, Faculty of Chemistry, Gdansk University of Technology, Narutowicza 11/12, 80-233 Gdansk, Poland
2
Department of Inorganic Chemistry, Faculty of Chemistry, Gdansk University of Technology, Narutowicza 11/12, 80-233 Gdansk, Poland
3
Department of Molecular Biology, Faculty of Biotechnology and Environment Sciences, The John Paul II Catholic University of Lublin, Konstantynów 1i, 20-708 Lublin, Poland
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceuticals 2020, 13(6), 111; https://doi.org/10.3390/ph13060111
Received: 29 April 2020 / Revised: 25 May 2020 / Accepted: 26 May 2020 / Published: 29 May 2020
(This article belongs to the Special Issue Design of Enzyme Inhibitors as Potential Drugs 2.0)
Five-membered 1,2,4-oxadiazole heterocyclic ring has received considerable attention because of its unique bioisosteric properties and an unusually wide spectrum of biological activities. Thus, it is a perfect framework for the novel drug development. After a century since the 1,2,4-oxadiazole have been discovered, the uncommon potential attracted medicinal chemists’ attention, leading to the discovery of a few presently accessible drugs containing 1,2,4-oxadiazole unit. It is worth noting that the interest in a 1,2,4-oxadiazoles’ biological application has been doubled in the last fifteen years. Herein, after a concise historical introduction, we present a comprehensive overview of the recent achievements in the synthesis of 1,2,4-oxadiazole-based compounds and the major advances in their biological applications in the period of the last five years as well as brief remarks on prospects for further development. View Full-Text
Keywords: 1,2,4-oxadiazole; synthetic methods; drug design; drug discovery; structure-activity relationship; medicinal application 1,2,4-oxadiazole; synthetic methods; drug design; drug discovery; structure-activity relationship; medicinal application
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MDPI and ACS Style

Biernacki, K.; Daśko, M.; Ciupak, O.; Kubiński, K.; Rachon, J.; Demkowicz, S. Novel 1,2,4-Oxadiazole Derivatives in Drug Discovery. Pharmaceuticals 2020, 13, 111.

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