Novel benzimidazole derivatives as effective inhibitors of prolyl oligopeptidase: synthesis, <i>in vitro and in silico</i> analysis-Reference-Cited by-同舟云学术

Novel benzimidazole derivatives as effective inhibitors of prolyl oligopeptidase: synthesis, in vitro and in silico analysis

Published:2024-01 Issue:1 Volume:16 Page:43-58
ISSN:1756-8919
Container-title:Future Medicinal Chemistry
language:en
Short-container-title:Future Medicinal Chemistry

Author:

Shakoor Abdul¹,Alam Aftab²,Jan Faheem³,Khan Momin¹,Ali Mumtaz²,Ullah Saeed⁴,Khan Ajmal⁴,AlAsmari Abdullah F⁵,Alasmari Fawaz⁵,Al-Ghafri Ahmed⁴,Al-Harrasi Ahmed⁴

Affiliation:

1. Department of Chemistry, Abdul Wali Khan University, Mardan, 23200, Pakistan

2. Department of Chemistry, University of Malakand, PO Box 18800, Khyber Pakhtunkhwa, Pakistan

3. Shenyang National Laboratory for Materials Science, Institute of Metal Research Chinese Academy of Sciences, Shenyang, Liaoning, 110016, People's Republic of China

4. Natural and Medical Sciences Research Center, University of Nizwa, PO Box 33, Nizwa, Oman

5. Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh, 11451, Saudi Arabia

Abstract

Background: This research aims to discover novel derivatives having potential therapeutic applications in treating conditions related to prolyl oligopeptidase (POP) dysfunction. Method: Novel benzimidazole derivatives have been synthesized, characterized and screened for their in vitro POP inhibition. Results: All these derivatives showed excellent-to-good inhibitory activities in the range of IC50 values of 3.61 ± 0.15 to 43.72 ± 1.18 μM, when compared with standard Z-prolyl-prolinal. The docking analysis revealed the strong interactions between our compounds and the target enzyme, providing critical insights into their binding affinities and potential implications for drug development. Conclusion: The significance of these compounds in targeting POP enzyme offers promising prospects for future research in the field of neuropharmacology.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

Link

https://www.future-science.com/doi/pdf/10.4155/fmc-2023-0267

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