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Novel substituted oxadiazole - piperazine derivatives as potential MAO inhibitors: Design, synthesis, in vitro and in silico studies

Year 2022, Volume: 26 Issue: 1, 20 - 27, 28.06.2025

Harun Uslu , Begüm Nurpelin Saglik , Derya Osmaniye , Kadriye Benkli

Abstract

Recent studies have shown that there are many piperazine and oxadiazole derivatives with MAO-A and/or MAO-B inhibitory activity. For this reason in our recent study, a new compound series of oxadiazole - piperazine derivatives (4a-e) were designed, synthesized, characterized and screened their hMAOs inhibitory activities. When the in silico studies were examined, it was seen that the pharmacokinetic properties and interactions with the receptor of synthesized compounds were suitable. Compound 4e, with a NO2 group on the 4-position of the phenyl ring, found showing significant MAO-A inhibitory activity. Compound 4e, was the most effective agent against MAO-A enzyme with IC50 value of 0.116 ± 0.004 μM. The newly synthesized oxadiazole - piperazine derivatives appears to be supported studies to design MAO inhibitors to obtain more suitable drugs, against diseases such as depression and anxiety due to MAO-A.

Keywords

hMAOs inhibition oxadiazole piperazine ADME molecular docking

References

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There are 29 citations in total.

Details

Primary Language English
Subjects Pharmaceutical Chemistry
Journal Section Articles
Authors

Harun Uslu

Begüm Nurpelin Saglik

Derya Osmaniye

Kadriye Benkli

Publication Date June 28, 2025
Published in Issue Year 2022 Volume: 26 Issue: 1

Cite

APA Uslu, H., Saglik, B. N., Osmaniye, D., Benkli, K. (2025). Novel substituted oxadiazole - piperazine derivatives as potential MAO inhibitors: Design, synthesis, in vitro and in silico studies. Journal of Research in Pharmacy, 26(1), 20-27.
AMA Uslu H, Saglik BN, Osmaniye D, Benkli K. Novel substituted oxadiazole - piperazine derivatives as potential MAO inhibitors: Design, synthesis, in vitro and in silico studies. J. Res. Pharm. June 2025;26(1):20-27.
Chicago Uslu, Harun, Begüm Nurpelin Saglik, Derya Osmaniye, and Kadriye Benkli. “Novel Substituted Oxadiazole - Piperazine Derivatives As Potential MAO Inhibitors: Design, Synthesis, in Vitro and in Silico Studies”. Journal of Research in Pharmacy 26, no. 1 (June 2025): 20-27.
EndNote Uslu H, Saglik BN, Osmaniye D, Benkli K (June 1, 2025) Novel substituted oxadiazole - piperazine derivatives as potential MAO inhibitors: Design, synthesis, in vitro and in silico studies. Journal of Research in Pharmacy 26 1 20–27.
IEEE H. Uslu, B. N. Saglik, D. Osmaniye, and K. Benkli, “Novel substituted oxadiazole - piperazine derivatives as potential MAO inhibitors: Design, synthesis, in vitro and in silico studies”, J. Res. Pharm., vol. 26, no. 1, pp. 20–27, 2025.
ISNAD Uslu, Harun et al. “Novel Substituted Oxadiazole - Piperazine Derivatives As Potential MAO Inhibitors: Design, Synthesis, in Vitro and in Silico Studies”. Journal of Research in Pharmacy 26/1 (June2025), 20-27.
JAMA Uslu H, Saglik BN, Osmaniye D, Benkli K. Novel substituted oxadiazole - piperazine derivatives as potential MAO inhibitors: Design, synthesis, in vitro and in silico studies. J. Res. Pharm. 2025;26:20–27.
MLA Uslu, Harun et al. “Novel Substituted Oxadiazole - Piperazine Derivatives As Potential MAO Inhibitors: Design, Synthesis, in Vitro and in Silico Studies”. Journal of Research in Pharmacy, vol. 26, no. 1, 2025, pp. 20-27.
Vancouver Uslu H, Saglik BN, Osmaniye D, Benkli K. Novel substituted oxadiazole - piperazine derivatives as potential MAO inhibitors: Design, synthesis, in vitro and in silico studies. J. Res. Pharm. 2025;26(1):20-7.