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用于新药研发的哌嗪支架:迄今的证据。

The piperazine scaffold for novel drug discovery efforts: the evidence to date.

作者信息

Romanelli Maria Novella, Manetti Dina, Braconi Laura, Dei Silvia, Gabellini Alessio, Teodori Elisabetta

机构信息

Department of Neuroscience, Psychology, Drug Research and Child's Health (NEUROFARBA), Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Sesto Fiorentino, Italy.

出版信息

Expert Opin Drug Discov. 2022 Sep;17(9):969-984. doi: 10.1080/17460441.2022.2103535. Epub 2022 Jul 28.

DOI:10.1080/17460441.2022.2103535
PMID:35848922
Abstract

INTRODUCTION

Piperazine is a structural element present in drugs belonging to various chemical classes and used for numerous different therapeutic applications; it has been considered a privileged scaffold for drug design.

AREAS COVERED

The authors have searched examples of piperazine-containing compounds among drugs recently approved by the FDA and in some research fields (nicotinic receptor modulators, compounds acting against cancer, and bacterial multidrug resistance), looking in particular to the design behind the insertion of this moiety.

EXPERT OPINION

Piperazine is widely used due to its peculiar characteristics, such as solubility, basicity, chemical reactivity, and conformational properties. This moiety has represented an important tool to modulate pharmacokinetic and pharmacodynamic properties of drugs.

摘要

引言

哌嗪是存在于多种化学类别的药物中的一种结构元素,用于众多不同的治疗应用;它被认为是药物设计的一个优势骨架。

涵盖领域

作者在最近被美国食品药品监督管理局(FDA)批准的药物以及一些研究领域(烟碱受体调节剂、抗癌化合物和细菌多药耐药性)中搜索了含哌嗪化合物的实例,特别关注该部分插入背后的设计。

专家观点

哌嗪因其独特的特性,如溶解性、碱性、化学反应性和构象性质而被广泛使用。该部分已成为调节药物药代动力学和药效学性质的重要工具。

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