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喹唑啉概述:药理学意义与最新进展。

An overview of quinazolines: Pharmacological significance and recent developments.

机构信息

Medicinal Chemistry Research Laboratory, MNR College of Pharmacy, Sangareddy, Gr.Hyderabad, 502 294, India.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sri Ramachandra Medical College & Research Institute (Deemed University), Porur, Chennai, 600 116, India.

出版信息

Eur J Med Chem. 2018 May 10;151:628-685. doi: 10.1016/j.ejmech.2018.03.076. Epub 2018 Mar 30.

Abstract

Most of the drugs and pharmacologically relevant molecules possess heterocyclic ring structures and presence of hetero atoms or groupings divulges privileged specificities in their pharmacological targets. Especially the heterocyclic systems, quinazoline is a biologically imperative scaffold known to be linked with several pharmacological activities. Some of the protuberant pharmacological responses attributed to this system are analgesic, anti-inflammatory, anti-convulsant, sedative-hypnotic, anti-histaminic, anti-hypertensive, anti-cancer, anti-microbial, anti-tubercular and anti-viral activities. This multiplicity in the pharmacological response contours of quinazoline has attracted the consideration of medicinal chemists to explore this system to its multiple potential against numerous activities. Several of these synthetic and pharmacological investigations have been successively studied for structure-activity relationship (SAR) to correlate the particular structural features for their pharmacological target. The emerging understanding of quinazoline derivatives on their pharmacological target offer opportunities for novel therapeutics. This review principally emphases on the medicinal chemistry aspects including drug design, structure-activity relationships (SARs), and mechanism of actions of quinazoline derivatives. This review gives detailed attention on in vitro and in vivo pharmacological activities of quinazoline and its analogs in the perspective of drug discovery and its development.

摘要

大多数药物和具有药理相关性的分子都具有杂环结构,杂原子或基团的存在揭示了其在药理靶点上的特权特异性。特别是杂环系统,喹唑啉是一种具有重要生物学意义的支架,与多种药理活性有关。该系统归因于一些突出的药理反应有镇痛、抗炎、抗惊厥、镇静催眠、抗组胺、抗高血压、抗癌、抗菌、抗结核和抗病毒活性。喹唑啉在药理反应轮廓上的这种多样性引起了药物化学家的关注,他们试图探索这一系统的多种潜在用途,以对抗多种活性。已经对这些合成和药理学研究进行了多次结构-活性关系(SAR)研究,以将特定的结构特征与其药理靶点相关联。对喹唑啉衍生物在其药理靶点上的认识为新型治疗方法提供了机会。这篇综述主要强调了包括药物设计、构效关系(SAR)和喹唑啉衍生物作用机制在内的药物化学方面。这篇综述从药物发现和开发的角度详细关注了喹唑啉及其类似物的体外和体内药理活性。

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