Babalola Benjamin Ayodipupo, Sharma Lekhnath, Olowokere Olanike, Malik Monika, Folajimi Oreoluwa
Department of Chemistry, Purdue University, 560 Oval Drive, IN 47907 West Lafayette, USA; Purdue Institute for Cancer Research, 201 S. University St., IN 47907 West Lafayette, USA.
Department of Chemistry, Indian Institute of Technology Indore Simrol, Khandwa Road, Indore, India.
Bioorg Med Chem. 2024 Oct 1;112:117876. doi: 10.1016/j.bmc.2024.117876. Epub 2024 Aug 16.
In this dispensation of rapid scientific and technological advancements, significant efforts are being made to curb health-related diseases. Research discoveries have highlighted the value of heterocyclic compounds, particularly thiadiazole derivatives, due to their diverse pharmacological activities. These compounds play a crucial role in therapeutic medicine and the development of effective drugs. Thiadiazoles are five-membered heterocyclic compounds consisting of one sulfur and two nitrogen atoms. This review explores advanced synthesis techniques, including the use of heterogeneous catalysts, microwave-assisted methods, ultrasound-assisted synthesis, solvent-free processes, multicomponent reactions, copper-catalyzed aerobic oxidative annulation, intramolecular cyclization, click-chemistry supported synthesis, and alkali-promoted, transition-metal-free mediated synthesis. These methods enhance the diversity and potential applications of thiadiazole compounds. Furthermore, this study provides up-to-date information on the key pharmacological activities of thiadiazole derivatives, highlighting their potential in therapeutic medicine for drug development. The structure-activity relationship (SAR) is also discussed to better understand their interactions and safety in biological systems. This work aims to expand on the reported chemistry and pharmacological potential of the thiadiazole moiety to validate their efficacy as promising pharmacophores in drug design and development.
在这个科技飞速发展的时代,人们正在做出巨大努力来控制与健康相关的疾病。研究发现突出了杂环化合物的价值,特别是噻二唑衍生物,因为它们具有多样的药理活性。这些化合物在治疗医学和有效药物的开发中起着至关重要的作用。噻二唑是由一个硫原子和两个氮原子组成的五元杂环化合物。本综述探讨了先进的合成技术,包括使用多相催化剂、微波辅助方法、超声辅助合成、无溶剂工艺、多组分反应、铜催化的有氧氧化环化、分子内环化、点击化学支持的合成以及碱促进的无过渡金属介导的合成。这些方法增强了噻二唑化合物的多样性和潜在应用。此外,本研究提供了关于噻二唑衍生物关键药理活性的最新信息,突出了它们在治疗医学药物开发中的潜力。还讨论了构效关系(SAR),以更好地理解它们在生物系统中的相互作用和安全性。这项工作旨在扩展已报道的噻二唑部分的化学和药理潜力,以验证它们作为药物设计和开发中有前景的药效基团的功效。