吡唑核是一种易于制备的支架,具有很大的治疗潜力。因此,寻找新的吡唑基化合物引起了学术界和工业界的极大兴趣。在过去的十年里,关于设计的大量论文和评论,合成,和不同类别的吡唑和许多含吡唑化合物的生物学评价已经发表。然而,在3、4或5位带有游离氨基的吡唑衍生物的概述(即,3-氨基吡唑,4-氨基吡唑,和5-氨基吡唑,分别),它们的生物学特性仍然缺失,尽管氨基吡唑是能够为受体或酶提供有用配体的有利框架,如p38MAPK,和不同的激酶,COX和其他,以及细菌和病毒感染的重要目标。为了填补这一空白,本综述侧重于在不同治疗领域作为活性剂研究的基于氨基吡唑的化合物,特别注意由每一类化合物定义的设计和结构-活性关系。特别是,抗癌/抗炎化合物获得了最相关的结果,正如最近批准的Pirtobrutinib所证明的那样。这里报告的数据是从不同的数据库收集的(Scifinder,WebofScience,Scopus,谷歌学者,并Pubmed)使用“氨基吡唑”作为关键字。
A pyrazole nucleus is an easy-to-prepare scaffold with large therapeutic potential. Consequently, the search for new pyrazole-based compounds is of great interest to the academic community as well as industry. In the last ten years, a large number of papers and reviews on the design, synthesis, and biological evaluation of different classes of pyrazoles and many pyrazole-containing compounds have been published. However, an overview of pyrazole derivatives bearing a free amino group at the 3, 4, or 5 position (namely, 3-aminopyrazoles, 4-aminopyrazoles, and 5-aminopyrazoles, respectively) and their biological properties is still missing, despite the fact that aminopyrazoles are advantageous frameworks able to provide useful ligands for receptors or enzymes, such as
p38MAPK, and different kinases, COX and others, as well as targets important for bacterial and virus infections. With the aim to fill this gap, the present
review focuses on aminopyrazole-based compounds studied as active agents in different therapeutic areas, with particular attention on the design and structure-activity relationships defined by each class of compounds. In particular, the most relevant results have been obtained for anticancer/anti-inflammatory compounds, as the recent approval of Pirtobrutinib demonstrates. The data reported here are collected from different databases (Scifinder, Web of Science, Scopus, Google Scholar, and Pubmed) using \"aminopyrazole\" as the keyword.