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Synthetic approaches, structure activity relationship and biological applications for pharmacologically attractive pyrazole/pyrazoline-thiazolidine-based hybrids

机译:具有药理吸引力的吡唑/吡唑啉-噻唑烷类杂化物的合成方法,结构活性关系和生物学应用

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摘要

The features of the chemistry of 4-thiazolidinone and pyrazole/pyrazolines as pharmacologically attractive scaffolds were described in a number of reviews in which the main approaches to the synthesis of mentioned heterocycles and their biological activity were analyzed. However, the pyrazole/pyrazoline thiazolidine-based hybrids as biologically active compounds is poorly discussed in the context of pharmacophore hybrid approach. Therefore, the purpose of this review is to summarize the data about the synthesis and modification of heterocyclic systems with thiazolidine and pyrazoline or pyrazole fragments in molecules as promising objects of modern bioorganic and medicinal chemistry. The description of biological activity was focused on SAR analysis and mechanistic insights of mentioned hybrids. (C) 2016 Elsevier Masson SAS. All rights reserved.
机译:在许多综述中描述了4-噻唑烷酮和吡唑/吡唑啉作为具有药理吸引力的支架的化学特征,其中分析了所述杂环的合成及其生物学活性的主要方法。但是,在药效基团杂合方法的背景下,作为生物活性化合物的吡唑/吡唑啉噻唑烷杂化物很少讨论。因此,本综述的目的是概述有关分子中噻唑烷和吡唑啉或吡唑片段作为现代生物有机和药物化学的有希望对象的杂环体系的合成和修饰的数据。生物活性的描述集中在SAR分析和提到的杂种的机理见解上。 (C)2016 Elsevier Masson SAS。版权所有。

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