ArticleMolecules (Basel, Switzerland)2026
Synthesis of 1,2,4-Oxadiazole Sulfonamide Derivatives and Their Biological Investigation as Monoamine Oxidase Inhibitors.
Anton A Shetnev, Olga A Gasilina, Sergey V Baykov, Rakhymzhan Turmanov, Nurbol Appazov, Rakhmetulla Zhapparbergenov, Nurila Togyzbayeva, Mikhail K Korsakov, Stephanus J Cloete, Anél Petzer and 1 more
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In one paragraphArticle in Molecules (Basel, Switzerland), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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11 authors.
Anton A ShetnevInstitute of Chemistry, Saint Petersburg State University, Universitetskaya Nab., 7/9, 199034 Saint Petersburg, Russia.ORCID 0000-0002-4389-461X Olga A GasilinaPharmaceutical Technology Transfer Centre, Yaroslavl State Pedagogical University Named After K. D. Ushinsky, Respublikanskaya St., 108, 150000 Yaroslavl, Russia.ORCID 0000-0001-9701-9207 Sergey V BaykovInstitute of Chemistry, Saint Petersburg State University, Universitetskaya Nab., 7/9, 199034 Saint Petersburg, Russia.ORCID 0000-0002-8912-5816 Rakhymzhan TurmanovLaboratory of Engineering Profile "Physical and Chemical Methods of Analysis", Korkyt Ata Kyzylorda University, 29 Aiteke bi Str., Kyzylorda 120000, Kazakhstan.ORCID 0000-0002-7268-1699 Nurbol AppazovLaboratory of Engineering Profile "Physical and Chemical Methods of Analysis", Korkyt Ata Kyzylorda University, 29 Aiteke bi Str., Kyzylorda 120000, Kazakhstan.ORCID 0000-0001-8765-3386 Rakhmetulla ZhapparbergenovLaboratory of Engineering Profile "Physical and Chemical Methods of Analysis", Korkyt Ata Kyzylorda University, 29 Aiteke bi Str., Kyzylorda 120000, Kazakhstan.ORCID 0000-0002-0567-3226 Nurila TogyzbayevaLaboratory of Engineering Profile "Physical and Chemical Methods of Analysis", Korkyt Ata Kyzylorda University, 29 Aiteke bi Str., Kyzylorda 120000, Kazakhstan.ORCID 0000-0003-4310-0661 Mikhail K KorsakovInstitute of Chemistry, Saint Petersburg State University, Universitetskaya Nab., 7/9, 199034 Saint Petersburg, Russia.ORCID 0000-0003-0913-2571 Stephanus J CloetePharmaceutical Chemistry and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa.ORCID 0000-0002-3770-8403 Anél PetzerPharmaceutical Chemistry and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa.ORCID 0000-0001-8114-8223 Jacobus P PetzerPharmaceutical Chemistry and Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom 2520, South Africa.ORCID 0000-0002-7114-8120 Funding
National Research Foundation of South Africa 137997Saint Petersburg State University 126022017742-6Science Committee of the Ministry of Science and Higher Education of the Republic of Kazakhstan AP23490015
6 · The paper itselfAbstract
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 IC
Indexed as
Monoamine OxidaseMonoamine Oxidase InhibitorsOxadiazolesSulfonamidesHumansMolecular StructureStructure-Activity Relationship1,2,4-oxadiazoleMonoamine OxidaseMonoamine Oxidase InhibitorsOxadiazolesSulfonamidesinhibitionMAOmonoamine oxidaseoxadiazoleParkinson’s diseasesulfonamide
Identifiers
PMID42796609
PMCPMC13610129
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