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喹唑啉-查尔酮和喹唑啉酮-查尔酮杂合体:生物活性的有前途的组合。

The Quinazoline-Chalcone and Quinazolinone-Chalcone Hybrids: A Promising Combination for Biological Activity.

机构信息

Laboratorio de Sínteses Organicas, Instituto de Quimica, Universidade Federal do Rio Grande do Sul, Av. Bento Goncalves 9500, CEP 91501-970, Agronomia, Porto Alegre, RS, Brazil.

出版信息

Mini Rev Med Chem. 2021;21(2):186-203. doi: 10.2174/1389557520666200730160325.

Abstract

Quinazoline and/or chalcones derivatives are important targets in several areas of chemical sciences, mainly, in the medicinal chemistry and pharmaceutical research. The purpose of this review was to systematize the information available in the literature, including patents, regarding the benefits, exerted by the combination of these two pharmacophores into single molecules. These hybrid compounds can exhibit different biological activities, causing a synergistic or a new effect, compared to the individuals. The variability of biological activities includes anticancer, anti-Alzheimer, antiviral and antimicrobial activities, among others. Additionally, synthetic methodologies to prepare the different molecular architectures were discussed based on their similarities. The increasing number of publications indicates the importance of molecular hybridization in the field of drug discovery.

摘要

喹唑啉和/或查耳酮衍生物是化学科学多个领域的重要目标,主要在药物化学和药物研究领域。本综述的目的是系统整理文献中关于将这两个药效团组合成单个分子的信息,包括专利。这些杂合化合物可以表现出不同的生物活性,与单独的化合物相比,产生协同或新的效果。生物活性的可变性包括抗癌、抗老年痴呆、抗病毒和抗菌活性等。此外,还根据其相似性讨论了制备不同分子结构的合成方法。越来越多的出版物表明分子杂交在药物发现领域的重要性。

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