当前位置: X-MOL 学术Lett. Drug Des. Discov. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis, Characterization and Antimicrobial Activity of Some Novel 1- substituted Benzimidazole Derivatives
Letters in Drug Design & Discovery ( IF 1.2 ) Pub Date : 2020-10-31 , DOI: 10.2174/1570180817999200531164230
Erkut Isik 1 , Demet Astley 1 , Seda Yuksekdanaci 2 , Ihsan Yasa 3
Affiliation  

Background: Benzimidazole derivatives are an important class of heterocyclic compounds in organic chemistry as they are related to a wide range of biological properties, including antimicrobial activity.

Methods: A series of 1-naphthoyl and benzoyl benzimidazole derivatives were synthesised, identified and screened for their antimicrobial activities against a number of different test organisms such as Escherichia coli, Pseudomonas aureginosa, Klebsiella pneumoniae, Staphylococcus aureus, Enterococcus faecalis, Bacillus cereus, Salmonella typhimurium, Candida albicans (yeast).

Results and Discussion: Benzimidazole derivatives (3a-d) were synthesised by using 4 different aminoacids. L-methionine, L-isoleucine, D-Phenylysine and L-Phenylamine as starting materials in the study. Experimental studies involve the use of benzimidazole derivatives (3a-d) of the selected amino acids to synthesize the benzoyl and naphthoyl derivatives of benzimidazole (4a-d, 5a-c). The structures of the synthesized compounds were confirmed by spectroscopic analyses (FTIR, 1HNMR, 13C-NMR) and elemental analysis.

Conclusion: In this study, only one compound (5a) showed a low MIC value against the eukaryotic microorganism C. albicans. The other six compounds showed higher antimicrobial activities against the prokaryotes C. albicans which is a normal flora in the mouth but is one of the organisms that cause infections leading to the weakening of the human immune system. Compound 5a is a candidate for future alternative antimicrobial drugs against C. albicans infections. In addition, compound 5a has a potential to be used as an inhibitor against P. aureginosa for the treatment of cystic fibrosis.



中文翻译:

一些新型的1-取代苯并咪唑衍生物的合成,表征和抗菌活性

背景:苯并咪唑衍生物是有机化学中重要的杂环化合物,因为它们与多种生物学特性(包括抗菌活性)有关。

方法:合成,鉴定和筛选了一系列1-萘甲酰基和苯甲酰基苯并咪唑衍生物对多种不同的测试微生物的抗菌活性,这些微生物例如大肠杆菌,金黄色假单胞菌,肺炎克雷伯菌,金黄色葡萄球菌,粪肠球菌,沙门氏杆菌鼠伤寒,白色念珠菌(酵母)。

结果与讨论:用4种不同的氨基酸合成了苯并咪唑衍生物(3a-d)。以L-蛋氨酸,L-异亮氨酸,D-苯基赖氨酸和L-苯基胺为起始原料。实验研究涉及使用所选氨基酸的苯并咪唑衍生物(3a-d)合成苯并咪唑(4a-d,5a-c)的苯甲酰基和萘甲酰基衍生物。通过光谱分析(FTIR,1HNMR,13C-NMR)和元素分析确认了合成化合物的结构。

结论:在这项研究中,只有一种化合物(5a)对真核微生物白色念珠菌的MIC值低。其他六种化合物对原核生物白色念珠菌显示较高的抗菌活性,白色念珠菌是口腔中的正常菌群,但却是引起感染导致人体免疫系统减弱的生物之一。化合物5a是未来针对白色念珠菌感染的替代抗菌药物的候选药物。另外,化合物5a有潜力用作抗金黄色葡萄球菌的抑制剂,用于治疗囊性纤维化。

更新日期:2020-10-30
down
wechat
bug