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Volume 31
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10.3390/molecules31183326
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Article

Synthesis of 1,2,4-Oxadiazole Sulfonamide Derivatives and Their Biological Investigation as Monoamine Oxidase Inhibitors

by
Anton A. Shetnev
1,2,
Olga A. Gasilina
2,
Sergey V. Baykov
1,
Rakhymzhan Turmanov
3,4,*,
Nurbol Appazov
3,5,
Rakhmetulla Zhapparbergenov
3,4,
Nurila Togyzbayeva
3,
Mikhail K. Korsakov
1,2,
Stephanus J. Cloete
6,
Anél Petzer
6 and
Jacobus P. Petzer
6,*
1
Institute of Chemistry, Saint Petersburg State University, Universitetskaya Nab., 7/9, 199034 Saint Petersburg, Russia
2
Pharmaceutical Technology Transfer Centre, Yaroslavl State Pedagogical University Named After K. D. Ushinsky, Respublikanskaya St., 108, 150000 Yaroslavl, Russia
3
Laboratory of Engineering Profile “Physical and Chemical Methods of Analysis”, Korkyt Ata Kyzylorda University, 29 Aiteke bi Str., Kyzylorda 120000, Kazakhstan
4
“DPS Kyzylorda” LLP, Amangeldy Imanov Str., 112A, Kyzylorda 120008, Kazakhstan
5
“CNEC’’ LLP, Dariger Ali Lane, 2, Kyzylorda 120001, Kazakhstan
6
Pharmaceutical Chemistry and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa
*
Authors to whom correspondence should be addressed.
Molecules 2026, 31(18), 3326; https://doi.org/10.3390/molecules31183326 (registering DOI)
Submission received: 21 August 2026 / Revised: 11 September 2026 / Accepted: 12 September 2026 / Published: 19 September 2026
(This article belongs to the Section Bioorganic Chemistry)
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Abstract

Monoamine oxidase (MAO) enzymes catalyze the catabolism of neurotransmitter amines, and MAO inhibitors are therefore of much clinical value. Based on the continued interest in MAO inhibitors, the present study examined the MAO inhibition properties of 1,2,4-oxadiazole sulfonamide derivatives. While we previously investigated benzenesulfonamides as MAO inhibitors, the incorporation of the 1,2,4-oxadiazole ring as the heteroaromatic ring is novel. 1,2,4-Oxadiazole sulfonamide derivatives were prepared from the corresponding carboxylic acids and amidoximes by an acylation–cyclization reaction under basic conditions, and MAO inhibition properties were determined using recombinant human enzymes. The derivatives potently inhibited MAO-B, with seven compounds exhibiting IC50 values lower than 0.02 µM. In contrast, comparatively weak MAO-A inhibition was observed with IC50 values greater than 6.04 µM. Mechanistic studies indicated that a representative compound acted as a reversible and competitive inhibitor. It may be concluded that 1,2,4-oxadiazole sulfonamide derivatives exhibit promising, isoform-selective MAO-B inhibition that may be of value for future therapeutic application.
Keywords: monoamine oxidase; MAO; oxadiazole; sulfonamide; inhibition; Parkinson’s disease monoamine oxidase; MAO; oxadiazole; sulfonamide; inhibition; Parkinson’s disease
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MDPI and ACS Style

Shetnev, A.A.; Gasilina, O.A.; Baykov, S.V.; Turmanov, R.; Appazov, N.; Zhapparbergenov, R.; Togyzbayeva, N.; Korsakov, M.K.; Cloete, S.J.; Petzer, A.; et al. Synthesis of 1,2,4-Oxadiazole Sulfonamide Derivatives and Their Biological Investigation as Monoamine Oxidase Inhibitors. Molecules 2026, 31, 3326. https://doi.org/10.3390/molecules31183326

AMA Style

Shetnev AA, Gasilina OA, Baykov SV, Turmanov R, Appazov N, Zhapparbergenov R, Togyzbayeva N, Korsakov MK, Cloete SJ, Petzer A, et al. Synthesis of 1,2,4-Oxadiazole Sulfonamide Derivatives and Their Biological Investigation as Monoamine Oxidase Inhibitors. Molecules. 2026; 31(18):3326. https://doi.org/10.3390/molecules31183326

Chicago/Turabian Style

Shetnev, Anton A., Olga A. Gasilina, Sergey V. Baykov, Rakhymzhan Turmanov, Nurbol Appazov, Rakhmetulla Zhapparbergenov, Nurila Togyzbayeva, Mikhail K. Korsakov, Stephanus J. Cloete, Anél Petzer, and et al. 2026. "Synthesis of 1,2,4-Oxadiazole Sulfonamide Derivatives and Their Biological Investigation as Monoamine Oxidase Inhibitors" Molecules 31, no. 18: 3326. https://doi.org/10.3390/molecules31183326

APA Style

Shetnev, A. A., Gasilina, O. A., Baykov, S. V., Turmanov, R., Appazov, N., Zhapparbergenov, R., Togyzbayeva, N., Korsakov, M. K., Cloete, S. J., Petzer, A., & Petzer, J. P. (2026). Synthesis of 1,2,4-Oxadiazole Sulfonamide Derivatives and Their Biological Investigation as Monoamine Oxidase Inhibitors. Molecules, 31(18), 3326. https://doi.org/10.3390/molecules31183326

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