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Inhibitory activities of indolizine derivatives: a patent review
Expert Opinion on Therapeutic Patents ( IF 5.4 ) Pub Date : 2020-08-01 , DOI: 10.1080/13543776.2020.1798402
Kamal M Dawood 1 , Ashraf A Abbas 1
Affiliation  

ABSTRACT Introduction Indolizines are structural isomers with indoles. Although several indole-based commercial drugs are available in the market, none of the indolizine-based drugs are available up-to-date. Natural and synthetic indolizines have a wide-range of pharmaceutical importance such as antitumor, antimycobacterial, antagonist, and antiproliferative activities. This prompted us to search and collect all possible data about the pharmacological importance of indolizine to open an avenue to the researchers in exploring more medicinal applications of such biologically important compounds. Areas covered The current review article covers the advancements in the biological and pharmacological activities of indolizine-based compounds during the last decade. The covered areas of this work involved anticancer, anti-HIV-1, anti-inflammatory, antimicrobial, anti-tubercular, larvicidal, anti-schizophrenia, CRTh2 antagonist’s activities in addition to enzymatic inhibitory activity. Expert opinion The discovery of indolizine drugs will be a major breakthrough as compared with their widely available drug-containing indole isosteres. Major work collected here was focused on anticancer, anti-tubercular, anti-inflammatory, and enzymatic inhibitory activities. The SAR study of the reported biologically active indolizines is summarized throughout the review whenever highlighted to the rationale the behavior of inhibitory action. Several indolizines with certain functions provided great enhancement in the therapeutic activities comparing with reference drugs.

中文翻译:

中氮茚衍生物的抑制活性:专利审查

摘要 引言 Indolizines 是吲哚的结构异构体。尽管市场上有几种基于吲哚的商业药物,但没有一种基于吲哚嗪的药物是最新的。天然和合成的中氮茚具有广泛的药学重要性,例如抗肿瘤、抗分枝杆菌、拮抗剂和抗增殖活性。这促使我们搜索和收集有关中氮茚药理重要性的所有可能数据,以便为研究人员探索此类具有重要生物学意义的化合物的更多药用应用开辟道路。涵盖的领域 当前的评论文章涵盖了过去十年中中氮茚类化合物在生物学和药理活性方面的进展。这项工作的涵盖领域包括抗癌、抗 HIV-1、抗炎、抗菌、抗结核、杀幼虫、抗精神分裂症、CRTh2拮抗剂的活性以及酶抑制活性。专家意见 中氮茚类药物的发现与其广泛使用的含吲哚等排体药物相比将是一个重大突破。这里收集的主要工作集中在抗癌、抗结核、抗炎和酶抑制活性。每当强调抑制作用行为的基本原理时,报告的生物活性中氮茚的 SAR 研究都会在整个审查过程中进行总结。几种具有一定功能的中氮茚类药物与参比药物相比,其治疗活性有了很大的提高。专家意见 中氮茚类药物的发现与其广泛使用的含吲哚等排体药物相比将是一个重大突破。这里收集的主要工作集中在抗癌、抗结核、抗炎和酶抑制活性。每当强调抑制作用行为的基本原理时,报告的生物活性中氮茚的 SAR 研究都会在整个审查过程中进行总结。几种具有一定功能的中氮茚类药物与参比药物相比,其治疗活性有了很大的提高。专家意见 中氮茚类药物的发现与其广泛使用的含吲哚等排体药物相比将是一个重大突破。这里收集的主要工作集中在抗癌、抗结核、抗炎和酶抑制活性。每当强调抑制作用行为的基本原理时,报告的生物活性中氮茚的 SAR 研究都会在整个审查过程中进行总结。几种具有一定功能的中氮茚类药物与参比药物相比,其治疗活性有了很大的提高。每当强调抑制作用行为的基本原理时,报告的生物活性中氮茚的 SAR 研究都会在整个审查过程中进行总结。几种具有一定功能的中氮茚类药物与参比药物相比,其治疗活性有了很大的提高。每当强调抑制作用行为的基本原理时,报告的生物活性中氮茚的 SAR 研究都会在整个审查过程中进行总结。几种具有一定功能的中氮茚类药物与参比药物相比,其治疗活性有了很大的提高。
更新日期:2020-08-01
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