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吡嗪衍生物:专利研究综述(2008 年至今)。

Pyrazine derivatives: a patent review (2008 - present).

机构信息

Universidade Federal do Rio de Janeiro, Chemistry Institute, Department of Organic Chemistry, 27930-560, Mácae-RJ, Brazil.

出版信息

Expert Opin Ther Pat. 2012 Sep;22(9):1033-51. doi: 10.1517/13543776.2012.714370. Epub 2012 Aug 6.

Abstract

INTRODUCTION

Pyrazines derivatives are well-known and important two-nitrogen-containing six-membered ring aromatic heterocyclic compounds and can carry substituents at one or more of the four ring carbon atoms. Pyrazines are a class of compounds that occur in nature and various methods have been worked out for their synthesis. A large number of pyrazine derivatives have been found to possess diverse pharmacological properties, which has caused an increasing interest by researchers in this core.

AREA COVERED

This review provides a comprehensive review of the pyrazines derivatives patented between the years 2008 to 2012 as potential active compounds. The patent databases SciFinder and esp@cenet were used to locate patent applications that were published between 2008 to present. Information from articles published was also included.

EXPERT OPINION

The diversity of pyrazines derivatives found in organisms in nature with different applications began to arouse the interest of research in this nucleus. The pyrazines derivatives have numerous prominent pharmacological effects, such as antibacterial, antifungal, antimycobacterial, anti-inflammatory, analgesic, anticancer for different types, antidiabetic, treatment for arteriosclerosis, antiviral. It's the time to conduct further studies aimed at rationalizing the biological activities found in order to develop more effective and clinically interesting compounds.

摘要

简介

吡嗪衍生物是众所周知的重要的含两个氮原子的六元环芳香杂环化合物,可以在四个环碳原子中的一个或多个上带有取代基。吡嗪是一类存在于自然界中的化合物,已经制定了各种方法来合成它们。大量的吡嗪衍生物被发现具有多种药理学特性,这引起了研究人员对这一核心的越来越多的兴趣。

涵盖领域

本综述提供了 2008 年至 2012 年间作为潜在活性化合物的吡嗪衍生物专利的全面综述。专利数据库 SciFinder 和 esp@cenet 用于定位 2008 年至今发表的专利申请。还包括从已发表的文章中获得的信息。

专家意见

自然界中不同应用的生物体中发现的吡嗪衍生物的多样性开始引起人们对这一核心的研究兴趣。吡嗪衍生物具有许多显著的药理学作用,如抗菌、抗真菌、抗分枝杆菌、抗炎、镇痛、抗肿瘤(不同类型)、抗糖尿病、治疗动脉硬化、抗病毒。现在是时候进行进一步的研究,旨在使发现的生物活性合理化,以开发更有效和临床上更有趣的化合物。

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