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作为抗分枝杆菌剂的苯并咪唑核心结构。

Benzimidazole-core as an antimycobacterial agent.

作者信息

Keri Rangappa S, Rajappa Chethana Kolambae, Patil Siddappa A, Nagaraja Bhari Mallanna

机构信息

Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Kanakapura, Ramanagaram, Bangalore 562112, India.

Centre for Nano and Material Sciences, Jain University, Jain Global Campus, Kanakapura, Ramanagaram, Bangalore 562112, India.

出版信息

Pharmacol Rep. 2016 Dec;68(6):1254-1265. doi: 10.1016/j.pharep.2016.08.002. Epub 2016 Aug 4.

Abstract

Mycobacterium tuberculosis (Mtb) is considered as one of the precarious bacterial infections around the world. Through a projected 8.7 million new tuberculosis (TB) cases and 1.4 million mortalities per annum, this deadly infection resulted insubstantial amount of human deaths than any other single organism bacterial infections. TB is one of India's most threatening human health problems and it accounts for approximately 33% of the global health issues. Subsequently, for TB there is an imperative need for the improvement of existing drug candidates with newer targets and specified mechanism of action. Within the wide spectra of heterocycles, benzimidazole and its substituted analogues were evidenced promising biological efficacies enabling them to perform as new drug or prodrug candidates. Exceptional structural features of this class of heterocycle and versatile biological applications made it a privileged structural backbone in new drug design and discovery. Majorly, 2,5- and 2,6-disubstituted benzimidazole derivatives shown to induce significant antiTB potential. To seek more insights on this unique feature of benzimidazole candidates, there is an urgency to assemble the recent advances in this promising area. This review presents an overview of the recent advancements and focuses on the structural features responsible for unique antiTB applications and compiled published reports on benzimidazole derivatives emphasizing on different approaches employed for their syntheses in order to help medicinal and clinical chemists in designing next generation, yet effective and safer antiTB candidates.

摘要

结核分枝杆菌(Mtb)被认为是全球最危险的细菌感染之一。据预测,每年有870万新增结核病(TB)病例和140万人死亡,这种致命感染导致的人类死亡数量比任何其他单一生物体细菌感染都要多。结核病是印度最威胁人类健康的问题之一,约占全球健康问题的33%。因此,迫切需要以新的靶点和特定的作用机制改进现有的候选药物。在广泛的杂环化合物中,苯并咪唑及其取代类似物已被证明具有良好的生物学功效,使其能够作为新药或前药候选物。这类杂环化合物的特殊结构特征和广泛的生物学应用使其成为新药设计和发现中的一个特权结构骨架。主要地,2,5-和2,6-二取代苯并咪唑衍生物显示出显著的抗结核潜力。为了更深入了解苯并咪唑候选物的这一独特特性,迫切需要汇总这一有前景领域的最新进展。本综述概述了最近的进展,重点关注负责独特抗结核应用的结构特征,并汇编了关于苯并咪唑衍生物的已发表报告,强调了用于其合成的不同方法,以帮助药物和临床化学家设计下一代有效且更安全的抗结核候选物。

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