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Novel benzimidazole-oxadiazole hybrid molecules as promising antimicrobial agents

机译：新型苯并咪唑 - 二唑杂化分子作为承诺的抗微生物剂

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摘要

In the present study, we describe the design and expeditious synthesis of novel 2-aryl-5-(3-aryl-[1,2,4]-oxadiazol-5-yl)-1-methyl-1H-benzo[d] imidazole hybrid molecules as promising antimicrobial agents. The core moiety 2-aryl-ethyl-1H-benzo[d] imidazole-5-carboxylate was efficiently synthesized by a rapid `one pot' nitro reductive cyclization reaction using sodium dithionite as reagent. All the compounds were screened for their antimicrobial activities and the active compounds were screened for their antitubercular activity against Mycobacterium tuberculosis H37Rv strain by the Microplate Alamar Blue Assay method. Compounds 8k, 8n, 8p and 8r exhibited potent anti-tubercular activity with MIC of 1.6 mu g mL(-1), which is two times more potent than the standard drugs pyrazinamide and ciprofloxacin and fourfold superior to streptomycin and isoniazid. Further, potent compounds were tested for their preliminary toxicity by hemolytic assay, where the compounds remain nontoxic even at higher concentration and showed good selectivity index. The investigation of cytotoxicity against normal embryonic kidney cell line HEK 293 by MTT assay showed IC50 value of more than 355 mu g mL(-1) for all the tested potent compounds. From the screening study, 8k, 8n, 8p and 8r emerged as strong candidates with potent antimicrobial activities and good ADME parameters. Attempts were also made to establish the structural activity relationships among the tested compounds.
机译：在本研究中，我们描述的设计和合成迅速新的2-芳基-5-（3-芳基 - [1,2,4]恶二唑-5-基）-1-甲基-1H-苯并[d]咪唑杂交分子作为有前途的抗微生物剂。核心部分的2-芳基乙基-1H-苯并[d]咪唑-5-羧酸甲酯高效地通过使用连二亚硫酸钠作为试剂快速`一锅”硝基还原环化反应合成。所有的化合物筛选它们的抗微生物活性和筛选了抵抗由微孔板阿尔玛蓝测定法的结核分枝杆菌菌株H37Rv的抗结核活性的活性化合物。化合物8K，8N，8P和8R表现出强效的抗结核病活性为1.6亩克毫升（-1），这是两个倍更有效比标准药物吡嗪酰胺和环丙沙星和四倍优于链霉素和异烟肼的MIC。此外，有效的化合物是用于通过溶血测定他们的初步毒性，其中该化合物保留无毒甚至在较高的浓度并表现出良好的选择性指数测试。针对在正常胚胎肾细胞系HEK 293细胞毒性通过MTT测定调查显示出大于355微米克毫升IC 50值（-1），所有测试的有效的化合物。从筛选研究，8K，8N，8P和8R成为强有力的候选人具有强大的抗菌作用和良好的ADME参数。尝试也作了建立测试化合物之间的结构活性关系。

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  • 来源
    《RSC Advances》 |2016年第10期|共14页
  • 作者

    Shruthi N.; Poojary Boja; Kumar Vasantha; Hussain Mumtaz Mohammed; Rai Vaishali M.; Pai Vinitha R.; Bhat Mahima; Revannasiddappa B. C.;

  • 作者单位

    Mangalore Univ Dept Chem Mangalagangothri 574199 Karnataka India;

    Mangalore Univ Dept Chem Mangalagangothri 574199 Karnataka India;

    Mangalore Univ Dept Chem Mangalagangothri 574199 Karnataka India;

    SJM Coll Pharm Dept Pharmaceut Chem Chitradurga 575501 Karnataka India;

    Yenepoya Univ Dept Biochem Mangalore 575018 Karnataka India;

    Yenepoya Univ Dept Biochem Mangalore 575018 Karnataka India;

    Mangalore Univ Dept Chem Mangalagangothri 574199 Karnataka India;

    NGSM Inst Pharmaceut Sci Dept Pharmacol Mangalore 575018 India;

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  • 正文语种 eng
  • 中图分类 化学;
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