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异香豆素研究二十年硕果累累(1997 - 2016年)的专利综述。

A patent review of two fruitful decades (1997-2016) of Isocoumarin research.

作者信息

Hussain Hidayat, Green Ivan R

机构信息

a UoN Chair of Oman's Medicinal Plants and Marine Natural Products , University of Nizwa , Nizwa , Sultanate of Oman.

b Center for Marine Biotechnology and Biomedicine , Scripps Institution of Oceanography, University of California-San Diego , La Jolla , CA 92093-0204 , USA.

出版信息

Expert Opin Ther Pat. 2017 Nov;27(11):1267-1275. doi: 10.1080/13543776.2017.1344220. Epub 2017 Jul 6.

Abstract

Isocoumarins comprise a six-membered oxygen heterocycle (α-pyranone) along with one aromatic ring and are known to possess interesting biological properties. During the last two decade (1997-2016), isocoumarin chemistry has attracted attention due to its biological and pharmaceutical effects viz., anticancer, anti-diabetic, antibacterial, antimalarial, and fungicidal effects. Areas covered: This review covers the patents on the therapeutic activities of natural and synthetic isocoumarins over the last two decades (1997-2016). Moreover a number of international patents related to natural and synthetic isocoumarins along with their biological effects will be presented and discussed. Although a large number of patents have been published during the period of the review, the aim of this review is to focus on those important patents specifically related to microbial diseases, cancer, malaria, and diabetes. Expert opinion: Isocoumarin and its synthetic analogs display a wide range of important pharmaceutical properties. Furthermore, isocoumarins have the potential to conjugate with other anticancer drugs which will synergistically increase the delivery and thus anticancer effects. Moreover, in order to get lead compounds, scientists should focus on the synthesis of halo and functionalized heterocyclic ring containing derivatives of isocoumarins as more potent drugs.

摘要

异香豆素包含一个六元氧杂环(α-吡喃酮)和一个芳环,并且已知具有有趣的生物学特性。在过去二十年(1997 - 2016年)中,异香豆素化学因其生物学和药学作用,即抗癌、抗糖尿病、抗菌、抗疟疾和杀真菌作用而受到关注。涵盖领域:本综述涵盖了过去二十年(1997 - 2016年)中关于天然和合成异香豆素治疗活性的专利。此外,还将展示和讨论一些与天然和合成异香豆素及其生物学效应相关的国际专利。尽管在综述期间已经发表了大量专利,但本综述的目的是关注那些与微生物疾病、癌症、疟疾和糖尿病特别相关的重要专利。专家观点:异香豆素及其合成类似物具有广泛的重要药学特性。此外,异香豆素有可能与其他抗癌药物共轭,从而协同增加药物递送并增强抗癌效果。此外,为了获得先导化合物,科学家们应专注于合成含卤和官能化杂环的异香豆素衍生物作为更有效的药物。

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