吡啶在药物化学中的作用及含吡啶支架BACE1抑制剂的设计

Pyridine Pub Date : 2018-07-18 DOI:10.5772/INTECHOPEN.74719
Y. Hamada
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引用次数: 48

摘要

吡啶是一种独特的芳香环。虽然吡啶在工业上被使用,但吡啶部分存在于许多天然产物中,如维生素、辅酶和生物碱,也存在于许多药物和杀虫剂中。吡啶基团因其碱度、水溶性、稳定性、氢键形成能力等特点,以及其小分子尺寸,常用于药物中。由于吡啶环可以作为胺、酰胺、含氮杂环和苯环的生物异构体,因此用吡啶取代它们在药物发现中具有重要意义。最近,我们通过基于硅构象结构的药物设计合成了一系列BACE1抑制剂,并发现了吡啶片段作为支架的重要作用。在本章中,我们描述了吡啶在药物化学中的重要作用,以及具有吡啶支架的β-分泌酶抑制剂用于治疗阿尔茨海默病的发展。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Role of Pyridines in Medicinal Chemistry and Design of BACE1 Inhibitors Possessing a Pyridine Scaffold
Pyridine is a unique aromatic ring. Although pyridines are used industrially, pyridine moieties are present in many natural products, such as vitamins, coenzymes, and alkaloids, and also in many drugs and pesticides. Pyridine moieties are often used in drugs because of their characteristics such as basicity, water solubility, stability, and hydrogen bond-forming ability, and their small molecular size. Because pyridine rings are able to act as the bioisosteres of amines, amides, heterocyclic rings containing nitrogen atoms, and benzene rings, their replacement by pyridine moieties is important in drug discovery. Recently, we synthesized a series of BACE1 inhibitors by in silico conformational structure-based drug design and found an important role of pyridine moiety as a scaffold. In this chapter, we describe the important role of pyridines in medicinal chemistry and the development of β-secretase inhibitors possessing a pyridine scaffold for the treatment of Alzheimer’s disease.
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