Department of Research and Scientific Communications, Isthmus Research and Publishing House, U-13, Near Badi Masjid, Pulpehlad Pur, New Delhi 110044, India.
Department of Pharmacognosy, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
Molecules. 2022 Jun 21;27(13):3994. doi: 10.3390/molecules27133994.
For many decades, the thiazole moiety has been an important heterocycle in the world of chemistry. The thiazole ring consists of sulfur and nitrogen in such a fashion that the pi (π) electrons are free to move from one bond to other bonds rendering aromatic ring properties. On account of its aromaticity, the ring has many reactive positions where donor-acceptor, nucleophilic, oxidation reactions, etc., may take place. Molecules containing a thiazole ring, when entering physiological systems, behave unpredictably and reset the system differently. These molecules may activate/stop the biochemical pathways and enzymes or stimulate/block the receptors in the biological systems. Therefore, medicinal chemists have been focusing their efforts on thiazole-bearing compounds in order to develop novel therapeutic agents for a variety of pathological conditions. This review attempts to inform the readers on three major classes of thiazole-bearing molecules: Thiazoles as treatment drugs, thiazoles in clinical trials, and thiazoles in preclinical and developmental stages. A compilation of preclinical and developmental thiazole-bearing molecules is presented, focusing on their brief synthetic description and preclinical studies relating to structure-based activity analysis. The authors expect that the current review may succeed in drawing the attention of medicinal chemists to finding new leads, which may later be translated into new drugs.
几十年来,噻唑基一直是化学领域中重要的杂环。噻唑环由硫和氮组成,使得π(π)电子可以自由地从一个键移动到另一个键,从而赋予芳香环的性质。由于其芳香性,该环有许多反应性位置,可能发生供体-受体、亲核、氧化等反应。含有噻唑环的分子进入生理系统时,会表现出不可预测的行为,并以不同的方式重置系统。这些分子可以激活/停止生化途径和酶,或者刺激/阻断生物系统中的受体。因此,药物化学家一直致力于研究含噻唑的化合物,以开发用于各种病理状况的新型治疗剂。本文综述试图向读者介绍三大类含噻唑的分子:噻唑作为治疗药物、临床试验中的噻唑和临床前和开发阶段的噻唑。本文介绍了临床前和开发阶段含噻唑的分子,重点介绍了它们的简要合成描述和与基于结构的活性分析相关的临床前研究。作者希望本综述能够成功地引起药物化学家的注意,找到新的先导化合物,这些化合物可能会被进一步转化为新药。