吲哚支架在药物发现中的治疗重要性综述。

Q3 Pharmacology, Toxicology and Pharmaceutics Current drug discovery technologies Pub Date : 2023-01-01 DOI:10.2174/1570163820666230505120553
Nishith Teraiya, Khushbu Agrawal, Tarun M Patel, Archita Patel, Samir Patel, Umang Shah, Shaileshkumar Shah, Khushman Rathod, Krupa Patel
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引用次数: 0

摘要

吲哚因其多种药理活性而被称为多功能杂环构建基块,在候选药物的竞争中很有可能成功。许多天然产物、生物碱和具有生物活性的杂环都含有吲哚作为有效成分。这些鼓励研究人员将其作为药物开发过程中的先导进行探索。目前的手稿将成为理解具有广泛药理活性的结构多样的吲哚衍生物的火炬手。目前的手稿描述了与标准品相比具有优异生物活性的中间体及其官能团。撰写这篇综述是为了帮助研究人员选择针对其目标的线索,同时也为设计具有增强潜力的药物设计中基于混合药效团的方法提供重要见解。目前对吲哚衍生物的结构与生物活性以及必需的药效团进行了综述。该讨论是在登革热、基孔肯雅(抗病毒)、抗高血压、利尿剂、免疫调节剂、中枢神经系统兴奋剂、抗高血压药、抗心律失常药、抗阿尔茨海默氏症和神经保护药等具有挑战性的靶点下进行的,还包括抗癌、抗结核、抗微生物、抗艾滋病毒、抗疟、抗炎、抗利什曼原虫、抗菊花和酶抑制剂。因此,这篇综述包括对吲哚衍生物的19个不同药理学靶标的讨论,这些靶标可用于获得基于配体的药物设计所需的广泛信息。这篇文章将指导研究人员选择、设计铅和药效团,以及使用吲哚部分的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.

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来源期刊
Current drug discovery technologies
Current drug discovery technologies Pharmacology, Toxicology and Pharmaceutics-Drug Discovery
CiteScore
3.70
自引率
0.00%
发文量
48
期刊介绍: Due to the plethora of new approaches being used in modern drug discovery by the pharmaceutical industry, Current Drug Discovery Technologies has been established to provide comprehensive overviews of all the major modern techniques and technologies used in drug design and discovery. The journal is the forum for publishing both original research papers and reviews describing novel approaches and cutting edge technologies used in all stages of drug discovery. The journal addresses the multidimensional challenges of drug discovery science including integration issues of the drug discovery process.
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