Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmaceutical Sciences, Eberhard Karls Universität Tübingen, Tübingen, Germany.
Arch Pharm (Weinheim). 2017 Dec;350(12). doi: 10.1002/ardp.201700258. Epub 2017 Nov 16.
2-Alkylsulfanyl-4(5)-aryl-5(4)-heteroarylimidazoles represent an important class of ATP-competitive protein kinase inhibitors, offering the possibility of multiple interactions with different regions of the target enzyme. The necessity of exploring the effects of diverse chemical decorations around the imidazole core prompted the design of several synthetic routes aimed at achieving both efficiency and flexibility. Additionally, the optimization of established protocols and the extensive use of transition metal-catalyzed cross-coupling reactions have been broadening the spectrum of preparative methodologies within the last decade. This review summarizes the progress in the development of synthetic strategies leading to 2-alkylsulfanyl-4(5)-aryl-5(4)-heteroarylimidazoles and 1-alkyl-2-alkylsulfanyl-4(5)-aryl-5(4)-heteroarylimidazoles and offers a glance at the biological activities of this class of compounds.
2-烷硫基-4(5)-芳基-5(4)-杂芳基咪唑类化合物是一类重要的 ATP 竞争性蛋白激酶抑制剂，它们有可能与靶酶的不同区域发生多种相互作用。为了探索咪唑核心周围不同化学修饰的影响，需要设计几种合成路线，以实现效率和灵活性。此外，在过去十年中，通过优化已建立的方案和广泛使用过渡金属催化交叉偶联反应，扩展了制备方法的范围。这篇综述总结了合成策略的发展进展，这些策略可得到 2-烷硫基-4(5)-芳基-5(4)-杂芳基咪唑类化合物和 1-烷基-2-烷硫基-4(5)-芳基-5(4)-杂芳基咪唑类化合物，并对该类化合物的生物活性进行了概述。
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