Preprint Short Note Version 1 Preserved in Portico This version is not peer-reviewed

3-(3,4-Dichlorophenyl)-5-(1H-indol-5-yl)-1,2,4-oxadiazole

Version 1 : Received: 12 December 2022 / Approved: 13 December 2022 / Online: 13 December 2022 (07:12:01 CET)

A peer-reviewed article of this Preprint also exists.

Efimova, J.A.; Shetnev, A.A.; Baykov, S.V.; Petzer, A.; Petzer, J.P. 3-(3,4-Dichlorophenyl)-5-(1H-indol-5-yl)-1,2,4-oxadiazole. Molbank 2023, 2023, M1552. Efimova, J.A.; Shetnev, A.A.; Baykov, S.V.; Petzer, A.; Petzer, J.P. 3-(3,4-Dichlorophenyl)-5-(1H-indol-5-yl)-1,2,4-oxadiazole. Molbank 2023, 2023, M1552.

Abstract

3-(3,4-Dichlorophenyl)-5-(1H-indol-5-yl)-1,2,4-oxadiazole was synthesized via the condensation of 3,4-dichlorobenzamidoxime and methyl 1H-indole-5-carboxylate using superbasic medium (NaOH/DMSO). The compound was tested as a potential inhibitor of human monoamine oxidase (MAO) A and B. It demonstrated notable inhibition with an IC50 value of 0.036 μM for MAO-B and isoform specificity. The product was characterized by 1H NMR, 13C NMR, and HRMS. In conclusion, the new active MAO-B inhibitor may serve as a candidate for the future discovery of therapeutic agents for neurodegenerative disorders such as Parkinson’s disease.

Keywords

monoamine oxidase; inhibitors; indole; 1,2,4-oxadiazole; drug research; neuroprotective drugs; Parkinson’s disease; MAO

Subject

Chemistry and Materials Science, Medicinal Chemistry

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