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胍类化合物的生物活性,2008-2012 年更新。

Biological activities of guanidine compounds, 2008 - 2012 update.

机构信息

Medical University of Gdańsk, Department of Chemical Technology of Drugs, Al. Gen. Hallera 107, 80-416 Gdańsk, Poland.

出版信息

Expert Opin Ther Pat. 2013 Aug;23(8):965-95. doi: 10.1517/13543776.2013.788645. Epub 2013 Apr 25.

Abstract

INTRODUCTION

Compounds incorporating guanidine moiety have found many practical applications in diverse areas of chemistry, such as nucleophilic organocatalysis, anion recognition and coordination chemistry. Moreover, guanidine functional group is found in natural products, pharmaceuticals and cosmetic ingredients produced by synthetic methods. Thus, knowledge of their biological activities and therapeutic uses is of utmost importance for researchers involved in drug discovery processes.

AREAS COVERED

In this review the authors highlight the continued development and therapeutic applications of newly synthesized guanidine-containing compounds including small peptides and peptidomimetics incorporating arginine. The review presents patents and patent applications filed in the years 2008 - 2012 with emphasis placed on new mechanisms of pharmacological action of guanidine derivatives.

EXPERT OPINION

While guanidines are often thought of as strong organic bases and compounds hydrophilic in nature, over the last 4 years there has been an enormous increase in discovery of new promising lead structures with guanidine core, suitable for development of potential drugs acting at central nervous system, anti-inflammatory agents, anti-diabetic and chemotherapeutic agents as well as cosmetics.

摘要

简介

胍基化合物在化学的多个领域,如亲核有机催化、阴离子识别和配位化学中都有广泛的应用。此外,胍基官能团存在于天然产物、药物和通过合成方法生产的化妆品成分中。因此,了解它们的生物活性和治疗用途对于参与药物发现过程的研究人员来说是至关重要的。

涵盖领域

在这篇综述中,作者强调了新合成的含胍化合物(包括精氨酸的小肽和肽模拟物)的持续发展和治疗应用。综述了 2008 年至 2012 年期间提交的专利和专利申请,重点介绍了胍衍生物药理作用的新机制。

专家意见

虽然胍通常被认为是强有机碱,性质亲水,但在过去的 4 年中,人们发现了大量具有胍核的新的有前途的先导结构,这些结构适合开发作用于中枢神经系统、抗炎、抗糖尿病和化疗药物以及化妆品的潜在药物。

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