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

doi:10.4155/fmc-2023-0267

IMR OpenIR

	*Novel benzimidazole derivatives as effective inhibitors of prolyl oligopeptidase: synthesis, in vitro and in silico* analysis**
	Shakoor, Abdul 1; Alam, Aftab 2; Jan, Faheem 3; Khan, Momin 1; Ali, Mumtaz 2; Ullah, Saeed 4; Khan, Ajmal 4; Alasmari, Abdullah F.5; Alasmari, Fawaz 5; Al-Ghafri, Ahmed 4; Al-Harrasi, Ahmed 4
通讯作者	Khan, Momin(mominkhan@awkum.edu.pk) ; Al-Harrasi, Ahmed(aharrasi@unizwa.edu.om)
	2023-12-06
发表期刊	FUTURE MEDICINAL CHEMISTRY
ISSN	1756-8919
页码	16
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.
关键词	benzimidazole HR-ESI-MS hydrazone-Schiff bases molecular docking NMR spectroscopy POP inhibitor propyl oligopeptidase
资助者	King Saud University, Riyadh, Saudi Arabia
DOI	10.4155/fmc-2023-0267
收录类别	SCI
语种	英语
资助项目	King Saud University, Riyadh, Saudi Arabia[RSP2023R235]
WOS研究方向	Pharmacology & Pharmacy
WOS类目	Chemistry, Medicinal
WOS记录号	WOS:001114541300001
出版者	Newlands Press Ltd
引用统计	被引频次：12[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/177154
专题	中国科学院金属研究所
通讯作者	Khan, Momin; Al-Harrasi, Ahmed
作者单位	1.Abdul Wali Khan Univ, Dept Chem, Mardan 23200, Pakistan 2.Univ Malakand, Dept Chem, POB 18800, Khyber Pakhtunkhwa, Pakistan 3.Chinese Acad Sci, Inst Met Res, Shenyang Natl Lab Mat Sci, Shenyang 110016, Liaoning, Peoples R China 4.Univ Nizwa, Nat & Med Sci Res Ctr, POB 33, Nizwa, Oman 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.