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Pyrazolotriazines: Biological activities, synthetic strategies and recent developments
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2021-06-10 , DOI: 10.1016/j.ejmech.2021.113537
Seyedeh Roya Alizadeh 1 , Mohammad Ali Ebrahimzadeh 1
Affiliation  

Heterocyclic compounds create an important class of molecules that demonstrates various chemical spaces for the definition of effective medicines. Many N-heterocycles display numerous biological activities. Among condensed heterocycles, pyrazolotriazine derivatives have received the attention of researchers owing to the extensive spectrum of biological activities. The reactivity of identified compounds was similar to the free azoles and triazines. The pyrazolotriazine scaffold exhibited antiasthma, antiinflammatory, anticancer, antithrombogenic activity and showed activity for major depression and pathological anxiety. Pyrazolotriazine derivatives also exhibited antibacterial, anticancer, antimetabolites, antidiabetic, antiamoebic, anticonvulsant, antiproliferative activity, human carbonic anhydrase inhibition, cyclin-dependent kinase 2 inhibition, tyrosinase and urease inhibition, MAO-B inhibition, TTK inhibition, thymidine phosphorylase inhibition, tubulin polymerization inhibition, protoporphyrinogen oxidase inhibition, GABAA agonistic activity, hCRF1 receptor antagonistic activity, and CGRP receptor antagonistic activity. This paper structurally categorized various pyrazolotriazines to isomeric classes into six groups that containing pyrazolo [1,5-d] [1,2,4] triazine, pyrazolo [5,1-c] [1,2,4] triazine, pyrazolo [3,4-e] [1,2,4] triazine, pyrazolo [4,3-e] [1,2,4] triazines, pyrazolo [1,5-a] [1,3,5] triazine, and pyrazolo [3,4-d] [1,2,3] triazine and expressed biological activity, the synthetic procedures for each class of pyrazolotriazines, structure-activity relationship and their mechanism of action. Generally, this review summarily indicated the past and present studies about the discovery of new lead compounds with good biological activity.



中文翻译:

吡唑并三嗪:生物活性、合成策略和最新进展

杂环化合物创造了一类重要的分子,它们展示了用于定义有效药物的各种化学空间。许多氮杂环表现出许多生物活性。在稠合杂环中,吡唑并三嗪衍生物因其广泛的生物活性而受到研究人员的关注。已鉴定化合物的反应性与游离唑类和三嗪类相似。吡唑并三嗪支架表现出抗哮喘、抗炎、抗癌、抗血栓形成的活性,并显示出对重度抑郁和病理性焦虑的活性。吡唑并三嗪衍生物还表现出抗菌、抗癌、抗代谢、抗糖尿病、抗阿米巴、抗惊厥、抗增殖活性、人碳酸酐酶抑制、细胞周期蛋白依赖性激酶 2 抑制、一个竞赛活动,hCRF1受体拮抗作用,并且CGRP受体拮抗活性。本文将各种吡唑并三嗪在结构上分为六组异构体类别,分别是吡唑并[ 1,5-d ][ 1,2,4 ]三嗪、吡唑并[ 5,1-c ][ 1,2,4 ]三嗪、吡唑并[ 3,4-e ] [ 1,2,4 ] 三嗪、吡唑并 [ 4,3-e ] [ 1,2,4 ] 三嗪、吡唑并 [ 1,5-a ] [ 1,3,5 ] 三嗪和吡唑并 [ 3,4-d ] [ 1,2,3] 三嗪和表达的生物活性、各类吡唑并三嗪的合成程序、构效关系及其作用机制。总的来说,这篇综述总结了过去和现在关于发现具有良好生物活性的新先导化合物的研究。

更新日期:2021-06-17
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