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

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

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

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

References

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Details

Primary Language

English

Subjects

Pharmaceutical Chemistry

Journal Section

Research Article

Authors

Harun Uslu ^*
Türkiye

Begüm Nurpelin Saglik
Türkiye

Derya Osmaniye
Türkiye

Kadriye Benkli
Türkiye

Publication Date

June 28, 2025

Submission Date

August 16, 2021

Acceptance Date

November 18, 2021

Published in Issue

Year 2022 Volume: 26 Number: 1

IZ

https://izlik.org/JA54SA65LH

Cite

RIS / Bibtex

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. https://izlik.org/JA54SA65LH

AMA

1.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):20-27. https://izlik.org/JA54SA65LH

Chicago

Uslu, Harun, Begüm Nurpelin Saglik, Derya Osmaniye, and Kadriye Benkli. 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. https://izlik.org/JA54SA65LH.

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

[1]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, June 2025, [Online]. Available: https://izlik.org/JA54SA65LH

ISNAD

Uslu, Harun - Saglik, Begüm Nurpelin - Osmaniye, Derya - Benkli, Kadriye. “Novel Substituted Oxadiazole - Piperazine Derivatives As Potential MAO Inhibitors: Design, Synthesis, in Vitro and in Silico Studies”. Journal of Research in Pharmacy 26/1 (June 1, 2025): 20-27. https://izlik.org/JA54SA65LH.

JAMA

1.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, June 2025, pp. 20-27, https://izlik.org/JA54SA65LH.

Vancouver

1.Harun Uslu, Begüm Nurpelin Saglik, Derya Osmaniye, Kadriye Benkli. Novel substituted oxadiazole - piperazine derivatives as potential MAO inhibitors: Design, synthesis, in vitro and in silico studies. J. Res. Pharm. [Internet]. 2025 Jun. 1;26(1):20-7. Available from: https://izlik.org/JA54SA65LH