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吡唑同系物作为抗菌、抗癌和抗疟药物的分子洞察。

A Molecular Insight into Pyrazole Congeners as Antimicrobial, Anticancer, and Antimalarial Agents.

机构信息

Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Erandwane, Pune 411038, Maharashtra, India.

Center of Innovation and Translational Research, Poona College of Pharmacy, Bhartiya Vidyapeeth, Pune 411038, India.

出版信息

Med Chem. 2022;18(10):1044-1059. doi: 10.2174/1573406418666220303150640.

Abstract

BACKGROUND

Pyrazole is a bioactive heterocyclic congener with numerous biological and pharmacological functionalities. Due to their multiple prospective applications, developing innovative and novel pyrazoles and analogs, revealing revolutionary methods for synthesizing this nucleus, investigating diverse potencies of that heterocycle, and exploring possible pyrazole applications are becoming increasingly relevant.

OBJECTIVES

Pyrazole scaffolds have been proven successful as antimicrobial, anticancer, and antimalarial therapeutics against multiple targets like DNA gyrase, topoisomerase IV, Hsp90, and several kinase enzymes. For this variability in the biotic zone, their moiety has gained the attention of many scientists interested in researching chemical and pharmacological profiles.

RESULTS

The review covers pyrazole scaffolds with a variety of biological functions and attempts to connect the structure-activity relationship. Multiple pyrazole analogs have been produced as lead compounds, and their activities have been evaluated.

CONCLUSION

The combination of pyrazole with other pharmacophores in a molecule might lead to novel potent therapeutic medicines, which could aid in the development of potent lead compounds.

摘要

背景

吡唑是一种具有多种生物和药理功能的生物活性杂环同系物。由于其具有多种潜在的应用,因此开发创新的新型吡唑及其类似物、揭示合成该核的革命性方法、研究该杂环的多种潜能以及探索可能的吡唑应用变得越来越重要。

目的

吡唑支架已被证明可成功用作抗菌、抗癌和抗疟疾治疗剂,针对多种靶标,如 DNA 回旋酶、拓扑异构酶 IV、Hsp90 和几种激酶酶。由于这种在生物区系中的多样性,其部分引起了许多对研究化学和药理学特性感兴趣的科学家的关注。

结果

该综述涵盖了具有多种生物学功能的吡唑支架,并试图建立结构-活性关系。已经产生了多种吡唑类似物作为先导化合物,并对其活性进行了评估。

结论

将吡唑与分子中的其他药效团结合可能会产生新型有效的治疗药物,这可能有助于开发有效的先导化合物。

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