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吲哚——药物研发中一个有前景的骨架。

Indoles - A promising scaffold for drug development.

作者信息

Sravanthi T V, Manju S L

机构信息

Organic Chemistry Division, School of Advanced Sciences, VIT University, Vellore 632014, Tamil Nadu, India.

Organic Chemistry Division, School of Advanced Sciences, VIT University, Vellore 632014, Tamil Nadu, India.

出版信息

Eur J Pharm Sci. 2016 Aug 25;91:1-10. doi: 10.1016/j.ejps.2016.05.025. Epub 2016 May 27.

Abstract

Generally, heterocycles occupy a prominent place in chemistry due to their wide range of applications in the fields of drug design, photochemistry, agrochemicals, dyes and so on. Among them, indole scaffolds have been found in most of the important synthetic drug molecules and paved a faithful way to develop effective targets. Privileged structures bind to multiple receptors with high affinity, thus aiding the development of novel biologically active compounds. Among the indole class of compounds, 2-arylindoles appear to be a most promising lead for drug development. The derivatives of 2-arylindoles exhibits antibacterial, anticancer, anti-oxidants, anti-inflammatory, anti-diabetic, antiviral, antiproliferative, antituberculosis activity, etc. This article would provide a clear knowledge on the wide-ranging biological activities of 2-arylindoles over the past two decades, which would be beneficial for the designing of more potent drug targets in order to compete with the existing drugs.

摘要

一般来说,杂环化合物因其在药物设计、光化学、农用化学品、染料等领域的广泛应用而在化学领域占据突出地位。其中,吲哚骨架存在于大多数重要的合成药物分子中,为开发有效的靶点铺平了可靠的道路。优势结构以高亲和力与多种受体结合,从而有助于新型生物活性化合物的开发。在吲哚类化合物中,2-芳基吲哚似乎是药物开发中最有前景的先导物。2-芳基吲哚的衍生物具有抗菌、抗癌、抗氧化、抗炎、抗糖尿病、抗病毒、抗增殖、抗结核活性等。本文将清晰介绍过去二十年来2-芳基吲哚广泛的生物活性,这将有助于设计更有效的药物靶点,以与现有药物竞争。

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