Novel benzimidazole derivatives as effective inhibitors of prolyl oligopeptidase: synthesis, in vitro and in silico analysis
文献类型：期刊论文
| 作者 | Shakoor, Abdul2; Alam, Aftab3; Jan, Faheem4; Khan, Momin2; Ali, Mumtaz3; Ullah, Saeed1; Khan, Ajmal1; Alasmari, Abdullah F.5; Alasmari, Fawaz5; Al-Ghafri, Ahmed1 |
| 刊名 | FUTURE MEDICINAL CHEMISTRY
 |
| 出版日期 | 2023-12-06 |
| 页码 | 16 |
| 关键词 | benzimidazole HR-ESI-MS hydrazone-Schiff bases molecular docking NMR spectroscopy POP inhibitor propyl oligopeptidase |
| ISSN号 | 1756-8919 |
| DOI | 10.4155/fmc-2023-0267 |
| 通讯作者 | Khan, Momin(mominkhan@awkum.edu.pk) ; Al-Harrasi, Ahmed(aharrasi@unizwa.edu.om) |
| 英文摘要 | 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 mu M, 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. |
| 资助项目 | King Saud University, Riyadh, Saudi Arabia[RSP2023R235] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001114541300001 |
| 出版者 | Newlands Press Ltd |
| 资助机构 | King Saud University, Riyadh, Saudi Arabia |
| 源URL | [http://ir.imr.ac.cn/handle/321006/177153]  |
| 专题 | 金属研究所_中国科学院金属研究所 |
| 通讯作者 | Khan, Momin; Al-Harrasi, Ahmed |
| 作者单位 | 1.Univ Nizwa, Nat & Med Sci Res Ctr, POB 33, Nizwa, Oman 2.Abdul Wali Khan Univ, Dept Chem, Mardan 23200, Pakistan 3.Univ Malakand, Dept Chem, POB 18800, Khyber Pakhtunkhwa, Pakistan 4.Chinese Acad Sci, Inst Met Res, Shenyang Natl Lab Mat Sci, Shenyang 110016, Liaoning, Peoples R China 5.King Saud Univ, Coll Pharm, Dept Pharmacol & Toxicol, Riyadh 11451, Saudi Arabia |
| 推荐引用方式 GB/T 7714 | Shakoor, Abdul,Alam, Aftab,Jan, Faheem,et al. Novel benzimidazole derivatives as effective inhibitors of prolyl oligopeptidase: synthesis, in vitro and in silico analysis[J]. FUTURE MEDICINAL CHEMISTRY,2023:16. |
| APA | Shakoor, Abdul.,Alam, Aftab.,Jan, Faheem.,Khan, Momin.,Ali, Mumtaz.,...&Al-Harrasi, Ahmed.(2023).Novel benzimidazole derivatives as effective inhibitors of prolyl oligopeptidase: synthesis, in vitro and in silico analysis.FUTURE MEDICINAL CHEMISTRY,16. |
| MLA | Shakoor, Abdul,et al."Novel benzimidazole derivatives as effective inhibitors of prolyl oligopeptidase: synthesis, in vitro and in silico analysis".FUTURE MEDICINAL CHEMISTRY (2023):16. |
入库方式： OAI收割
来源：金属研究所
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