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

Julia A. Efimova; Anton A. Shetnev; Sergey V. Baykov; Anél Petzer; Jacobus P. Petzer

doi:10.20944/preprints202212.0230.v1

Submitted:

12 December 2022

Posted:

13 December 2022

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

Julia A. Efimova

,Anton A. Shetnev^*,Sergey V. Baykov,Anél Petzer,Jacobus P. Petzer

Julia A. Efimova

,Anton A. Shetnev^*,Sergey V. Baykov,Anél Petzer,Jacobus P. Petzer

A peer-reviewed article of this preprint also exists.

Submitted:

12 December 2022

Posted:

13 December 2022

You are already at the latest version

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

;

4-oxadiazole

;

drug research

;

neuroprotective drugs

;

Parkinson’s disease

;

MAO

Subject:

Chemistry and Materials Science - Medicinal Chemistry

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