Letters in Drug Design & Discovery ( IF 1.2 ) Pub Date : 2020-10-31 , DOI: 10.2174/1570180817999200523181211 Serry A. El Bialy 1 , Basem Mansour 1 , Waleed A. Bayoumi 1 , Amira Taman 2 , Hassan M. Eissaa 2
Background: Literature survey has pointed out that Benzimidazoles represent an interesting class of anthelmintics, of which several potent members were developed.
Objective: Benzimidazoles hybridized with pharmacophoric moieties possessing anthelmintic activity were designed, synthesized to be evaluated against cercaria.
Methods: Structural modification was achieved through 2- and 5-positions. Moreover, an in vitro cercarial assay was adopted to evaluate target compounds.
Results and Discussions: Biological screening revealed that compound 3h showed significant activity with a survival index of 35% at a 100 μg/mL concentration. Whereas, compounds 3a and 3c showed moderate activity, the rest of the tested compounds exhibited low activity.
Conclusion: The current study evidenced that the new hybrids "benzimidazole-thiophen-aryl" are successful as cercacidal agents. Further studies of this novel tri-ring system are suggested on adult worms of S. mansoni.
中文翻译:
新型2-(5-芳基)噻吩-2-基)苯并咪唑; 曼氏血吸虫尾核期的设计,合成及体外评价
背景:文献调查指出,苯并咪唑代表了一种令人关注的驱虫药,其中已开发出多种强效驱虫药。
目的:设计与具有驱虫活性的药效基团部分杂交的苯并咪唑类化合物,合成其对尾c的评价。
方法:通过2位和5位进行结构修饰。此外,采用体外尾car测定法评估目标化合物。
结果与讨论:生物筛选显示,化合物3h在100μg/ mL浓度下显示出显着的活性,存活指数为35%。而化合物3a和3c表现出中等活性,其余受试化合物则表现出低活性。
结论:目前的研究证明,新的杂种“苯并咪唑-噻吩-芳基”可以成功地用作脑酸剂。建议在曼氏沙门氏菌的成虫上对该新颖的三环系统进行进一步研究。