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基于吡唑骨架的神经保护剂的最新进展:综述。

Recent Advancement of Pyrazole Scaffold Based Neuroprotective Agents: A Review.

机构信息

Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka-576104, India.

Manipal McGill Centre for Infectious Diseases, Prasanna School of Public Health, Manipal Academy of Higher Education, Manipal, Karnataka-576104, India.

出版信息

CNS Neurol Disord Drug Targets. 2022;21(10):940-951. doi: 10.2174/1871527320666210602152308.

Abstract

As a source of therapeutic agents, heterocyclic nitrogen-containing compounds and their derivatives are still interesting and essential. Pyrazole, a five-member heteroaromatic ring with two nitrogen atoms, has a major impact in chemical industries as well as pharmaceutical industries. Due to its wide range of biological activities against various diseases, it has been identified as a biologically important heterocyclic scaffold. The treatment of neurological disorders has always been a difficult task in both the past and present. Therefore, identifying therapeutically effective molecules for neurological conditions remains an open challenge in biomedical research and development. For developing novel entities as neuroprotective agents, recently, pyrazole scaffold has attracted medicinal chemists worldwide. The major focus of research in this area is discovering novel molecules as neuroprotective agents with minimal adverse effects and better effectiveness in improving the neurological condition. This review mainly covers recent developments in the neuropharmacological role of pyrazole incorporated compounds, including their structural-activity relationship (SAR), which also further includes IC values (in mM as well as in μM), recent patents, and a brief history as neuroprotective agents.

摘要

作为治疗剂的来源,含杂环氮原子的化合物及其衍生物仍然是有趣且必不可少的。吡唑是一种含有两个氮原子的五元杂芳环,在化学工业和制药工业中都具有重要影响。由于其对各种疾病具有广泛的生物活性,因此被认为是一种具有重要生物学意义的杂环支架。治疗神经紊乱一直是过去和现在的一项艰巨任务。因此,寻找治疗神经疾病的有效分子仍然是生物医学研究和开发中的一个开放性挑战。为了开发新型的神经保护剂,最近,吡唑骨架已引起全球药物化学家的关注。该领域研究的主要重点是发现具有最小副作用和更好改善神经状况效果的新型分子作为神经保护剂。本篇综述主要涵盖了含吡唑化合物的神经药理学作用的最新进展,包括其构效关系(SAR),其中还包括 IC 值(以 mM 和 μM 表示)、最新专利和作为神经保护剂的简要历史。

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