Suppr超能文献

唑类支架的治疗潜力:专利研究综述(2006-2017)。

Therapeutic potential of oxazole scaffold: a patent review (2006-2017).

机构信息

a University Institute of Pharmaceutical Sciences, Panjab University , Chandigarh , India.

b Department of Chemistry , Panjab University , Chandigarh , India.

出版信息

Expert Opin Ther Pat. 2018 Nov;28(11):783-812. doi: 10.1080/13543776.2018.1526280. Epub 2018 Sep 26.

Abstract

INTRODUCTION

Oxazoles are oxygen and nitrogen containing five membered heterocyclic ring systems that are present in various anticancer, antimicrobial, antihyperglycemic, anti-inflammatory agents etc. of natural origin. These pharmacologically active oxazole derivatives have attracted numerous researchers to explore this scaffold for the design and development of newer potential therapeutic agents. A large number of synthetic oxazole containing molecules have been reported over the period that exhibited wide spectrum of pharmacological profiles. Some of them have shown promising therapeutic potential and have qualified for both preclinical and clinical evaluations.

AREAS COVERED

In this review, the patents (published during 2006-2017) focusing on the biological potential of oxazoles have been covered. Therapeutic applications and various techniques/assays employed for the in vitro/in vivo evaluation of patented derivatives have been discussed majorly.

EXPERT OPINION

Chemically oxazole offers three positions for substitution. These substituted oxazole derivatives of natural as well as synthetic origin have numerous pharmacological applications including anticancer, anti-Alzheimer's, anti-hyperglycemic, anti-inflammatory, antibacterial etc. Their pharmacological actions are mainly mediated through enzyme/receptor involved in the particular disease. The flexible nature of this ligand for various molecular level targets (enzyme/receptor) make this heterocylce an attractive scaffold for development of effective and clinically relevant oxazole containing therapeutic agents.

摘要

简介

恶唑是含有氧和氮的五元杂环系统,存在于各种天然来源的抗癌、抗菌、抗高血糖、抗炎等药物中。这些具有药理活性的恶唑衍生物吸引了众多研究人员探索这一支架,以设计和开发新的潜在治疗药物。在过去的一段时间里,已经报道了大量含有恶唑的合成分子,它们表现出广泛的药理特性。其中一些已经显示出有希望的治疗潜力,并已通过临床前和临床评估。

涵盖领域

本综述涵盖了 2006 年至 2017 年期间发表的专注于恶唑生物潜力的专利。主要讨论了专利衍生物的体外/体内评估所采用的治疗应用和各种技术/测定法。

专家意见

从化学角度来看,恶唑提供了三个可取代的位置。这些天然和合成来源的取代恶唑衍生物具有许多药理作用,包括抗癌、抗老年痴呆症、抗高血糖、抗炎、抗菌等。它们的药理作用主要是通过参与特定疾病的酶/受体来介导的。这种配体对各种分子水平靶标(酶/受体)的灵活性使其成为开发有效和临床相关的含恶唑治疗药物的有吸引力的支架。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验