CIHIDECAR-CONICET-Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Pabellón 2 - Ciudad Universitaria, 1428 Buenos Aires, Argentina.
Departamento de Ingeniería Química, Instituto Tecnológico de Buenos Aires, Av. Eduardo Madero 399, 1106 Buenos Aires, Argentina.
Eur J Med Chem. 2015 Jan 27;90:666-83. doi: 10.1016/j.ejmech.2014.12.012. Epub 2014 Dec 8.
Fused heterobicyclic systems have gained much importance in the field of medicinal chemistry because of their broad spectrum of physiological activities. Among the heterocyclic rings containing bridgehead nitrogen atom, imidazothiazoles derivatives are especially attractive because of their different biological activities. Since many imidazothiazoles derivatives are effective for treating several diseases, is interesting to analyze the behavior of some isosteric related heterocycles, such as pirrolothiazoles, imidazothiadiazoles and imidazotriazoles. In this context, this review summarizes the current knowledge about the syntheses and biological behavior of these families of heterocycles. Traditional synthetic methodologies as well as alternative synthetic procedures are described. Among these last methodologies, the use of multicomponent reaction, novel and efficient coupling reagents, and environmental friendly strategies, like microwave assistance and solvent-free condition in ionic liquids are also summarized. This review includes the biological assessments, docking research and studies of mechanism of action performed in order to obtain the compounds leading to the development of new drugs.
稠合杂环系统因其广泛的生理活性在药物化学领域中得到了广泛的重视。在含有桥头氮原子的杂环中，咪唑并噻唑衍生物因其不同的生物活性而特别引人注目。由于许多咪唑并噻唑衍生物对治疗多种疾病有效，因此分析一些等排相关杂环（如吡咯并噻唑、咪唑并噻二唑和咪唑并三唑）的行为很有趣。在这方面，本综述总结了这些杂环家族的合成和生物行为的最新知识。描述了传统的合成方法以及替代的合成方法。在这些最后方法中，还总结了多组分反应、新型高效偶联试剂以及环境友好策略（如微波辅助和离子液体中的无溶剂条件）的使用。本综述包括为了获得导致开发新药的化合物而进行的生物评估、对接研究和作用机制研究。
