吲哚支架在药物发现中的治疗重要性综述,Current Drug Discovery Technologies

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吲哚支架在药物发现中的治疗重要性综述
Current Drug Discovery Technologies Pub Date : 2023-07-05 , DOI: 10.2174/1570163820666230505120553
Nishith Teraiya ₁ , Khushbu Agrawal ₂ , Tarun M Patel ₃ , Archita Patel ₄ , Samir Patel ₄ , Umang Shah ₄ , Shaileshkumar Shah ₅ , Khushman Rathod ₁ , Krupa Patel ₁

Affiliation

吲哚因其多种药理活性而被称为多功能杂环结构单元，并且在候选药物的竞争中具有很高的成功概率。许多天然产物、生物碱和生物活性杂环化合物都含有吲哚作为活性成分药效基团。这些鼓励研究人员将其作为药物开发过程的先导进行探索。当前的手稿将成为了解具有广泛药理活性的结构多样的吲哚衍生物类别的火炬手。目前的手稿描述了与标准相比具有优异生物活性的中间体及其官能团。该综述旨在帮助研究人员针对其目标选择先导化合物，同时也为具有增强潜力的药物设计中基于混合药效基团的方法的设计提供重要的见解。目前对吲哚衍生物的综述将其结构与生物活性以及重要的药效团相关联，这一点得到了强调。讨论的主题包括登革热、基孔肯雅热（抗病毒）、抗高血压、利尿剂、免疫调节剂、中枢神经系统兴奋剂、降血脂、抗心律失常、抗阿尔茨海默病和神经保护，以及抗癌、抗结核、抗菌、抗艾滋病毒、抗疟疾等。、抗炎药、抗利什曼药、抗虫药和酶抑制剂。因此，本综述讨论了吲哚衍生物的 19 种不同药理学靶点，这些靶点可用于获取基于配体的药物设计所需的广泛信息。本文将指导研究人员选择、设计先导化合物和药效基团，以及使用吲哚部分进行基于配体的药物设计。

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A Review of the Therapeutic Importance of Indole Scaffold in Drug Discovery

Indole is known as a versatile heterocyclic building block for its multiple pharmacological activities and has a high probability of success in the race for drug candidates. Many natural products, alkaloids, and bioactive heterocycles contain indole as the active principle pharmacophore. These encourage the researchers to explore it as a lead in the drug development process. The current manuscript will serve as a torchbearer for understanding the structurally diverse class of indole derivatives with extensive pharmacological activity. The current manuscript describes the intermediates and their functional groups responsible for superior biological activity compared to the standard. The review is written to help researchers to choose leads against their target but also to provide crucial insight into the design of a hybrid pharmacophore-based approach in drug design with enhanced potential. The present reviews on the indole derivatives correlate the structures with biological activities as well as essential pharmacophores, which were highlighted. The discussion was explored under challenging targets like dengue, chikungunya (anti-viral), antihypertensive, diuretic, immunomodulator, CNS stimulant, antihyperlipidemic, antiarrhythmic, anti-Alzheimer’s, and neuroprotective, along with anticancer, antitubercular, antimicrobial, anti-HIV, antimalarial, anti-inflammatory, antileishmanial, antianthelmintic, and enzyme inhibitors. So, this review includes a discussion of 19 different pharmacological targets for indole derivatives that could be utilized to derive extensive information needed for ligand-based drug design. The article will guide the researchers in the selection, design of lead and pharmacophore, and ligand-based drug design using indole moiety.

更新日期：2023-07-05

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