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分子杂交:新药原型设计中的一种有用工具。

Molecular hybridization: a useful tool in the design of new drug prototypes.

作者信息

Viegas-Junior Cláudio, Danuello Amanda, da Silva Bolzani Vanderlan, Barreiro Eliezer J, Fraga Carlos Alberto Manssour

机构信息

Instituto de Química, Universidade Estadual Paulista Júlio de Mesquita Filho, Araraquara, São Paulo, SP, Brazil.

出版信息

Curr Med Chem. 2007;14(17):1829-52. doi: 10.2174/092986707781058805.

DOI:10.2174/092986707781058805
PMID:17627520
Abstract

Molecular hybridization is a new concept in drug design and development based on the combination of pharmacophoric moieties of different bioactive substances to produce a new hybrid compound with improved affinity and efficacy, when compared to the parent drugs. Additionally, this strategy can result in compounds presenting modified selectivity profile, different and/or dual modes of action and reduced undesired side effects. So, in this paper, we described several examples of different strategies for drug design, discovery and pharmacomodulation focused on new innovative hybrid compounds presenting analgesic, anti-inflammatory, platelet anti-aggregating, anti-infectious, anticancer, cardio- and neuroactive properties.

摘要

分子杂交是药物设计与开发中的一个新概念,它基于不同生物活性物质的药效基团组合,以产生一种新的杂合化合物。与母体药物相比,该杂合化合物具有更高的亲和力和疗效。此外,这种策略可使化合物呈现出改变的选择性概况、不同和/或双重作用模式,并减少不良副作用。因此,在本文中,我们描述了几种药物设计、发现和药效调节的不同策略实例,这些策略聚焦于具有镇痛、抗炎、抗血小板聚集、抗感染、抗癌、心血管和神经活性特性的新型创新杂合化合物。

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