Pharmacological and Toxicological Screening of Novel Benzimidazole-Morpholine Derivatives as Dual-Acting Inhibitors

被引：20

作者：

Can, Nafiz Oncu ^{[1
,2
]}

Cevik, Ulviye Acar ^{[2
,3
]}

Saglik, Begum Nurpelin ^{[2
,3
]}

Ozkay, Yusuf ^{[2
,3
]}

Atli, Ozlem ^{[4
]}

Baysal, Merve ^{[4
]}

Ozkay, Ulmide Demir ^{[5
]}

Can, Ozgur Devrim ^{[5
]}

机构：

[1] Anadolu Univ, Dept Analyt Chem, Fac Pharm, TR-26470 Eskisehir, Turkey

[2] Anadolu Univ, Doping & Narcot Cpds Anal Lab, Fac Pharm, TR-26470 Eskisehir, Turkey

[3] Anadolu Univ, Dept Pharmaceut Chem, Fac Pharm, TR-26470 Eskisehir, Turkey

[4] Anadolu Univ, Dept Pharmaceut Toxicol, Fac Pharm, TR-26470 Eskisehir, Turkey

[5] Anadolu Univ, Dept Pharmacol, Fac Pharm, TR-26470 Eskisehir, Turkey

来源：

MOLECULES | 2017年 / 22卷 / 08期

关键词：

benzimidazoles; morpholines; AChE; MAO; COX; MONOAMINE-OXIDASE-B; ANTIMICROBIAL ACTIVITY; BIOLOGICAL EVALUATION; AGENTS; DESIGN; BEARING; MOIETY; ASSAY;

D O I：

10.3390/molecules22081374

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The aim of this study was to investigate acetylcholinesterase (AChE), monoamine oxidase A (MAO-A), monoamine oxidase B (MAO-B), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzyme inhibitory, and antimicrobial activities of a new series of 2-(4-substituted phenyl)-1-[2-(morpholin-4-yl)ethyl]-1H-benzimidazole derivatives, for their possible use as multi-action therapeutic agents. Target compounds (n = 15) were synthesized under microwave irradiation conditions in two steps, and their structures were elucidated by FT-IR, H-1-NMR, C-13-NMR and high resolution mass spectroscopic analyses. Pharmacological screening studies revealed that two of the compounds (2b and 2j) have inhibitory potential on both COX-1 and COX-2 enzymes. In addition, cytotoxic and genotoxic properties of the compounds 2b, 2j and 2m were investigated via the well-known MTT and Ames tests, which revealed that the mentioned compounds are non-cytotoxic and non-genotoxic. As a concise conclusion, two novel compounds were characterized as potential candidates for treatment of frequently encountered inflammatory diseases.

引用

页数：20

共 63 条

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