Mishra Chandra Bhushan, Kumari Shikha, Tiwari Manisha
Bio-Organic Chemistry Laboratory, Dr. B.R. Ambedkar Center for Biomedical Research, University of Delhi, India.
Bio-Organic Chemistry Laboratory, Dr. B.R. Ambedkar Center for Biomedical Research, University of Delhi, India.
Eur J Med Chem. 2015 Mar 6;92:1-34. doi: 10.1016/j.ejmech.2014.12.031. Epub 2014 Dec 19.
Thiazole is a valuable scaffold in the field of medicinal chemistry and has accounted to display a variety of biological activities. Thiazole and its derivatives have attracted continuing interest to design various novel CNS active agents. In the past few decades, thiazoles have been widely used to develop a variety of therapeutic agents against numerous CNS targets. Thiazole containing drug molecules are currently being used in treatment of various CNS disorders and a number of thiazole derivatives are also presently in clinical trials. A lot of research has been carried out on thiazole and their analogues, which has proved their efficacy to overcome several CNS disorders in rodent as well as primate models. The aim of present review is to highlights diverse CNS activities displayed by thiazole and their derivatives. SAR of this nucleus has also been well discussed. This review covers the recent updates present in literature and will surely provide a greater insight for the designing and development of potent thiazole based CNS active agents in future.
噻唑是药物化学领域一种有价值的骨架结构，已被证明具有多种生物活性。噻唑及其衍生物一直吸引着人们持续关注，以设计各种新型中枢神经系统（CNS）活性剂。在过去几十年中，噻唑已被广泛用于开发针对众多中枢神经系统靶点的各种治疗剂。含噻唑的药物分子目前正用于治疗各种中枢神经系统疾病，并且许多噻唑衍生物目前也正在进行临床试验。对噻唑及其类似物已经进行了大量研究，这已证明它们在啮齿动物和灵长类动物模型中克服多种中枢神经系统疾病的功效。本综述的目的是突出噻唑及其衍生物所表现出的多种中枢神经系统活性。该核心结构的构效关系也已得到充分讨论。本综述涵盖了文献中的最新进展，肯定会为未来设计和开发有效的基于噻唑的中枢神经系统活性剂提供更深入的见解。
