Department of Chemistry, Kurukshetra University, Kurukshetra, 136 119, India.
CSIR-National Institute of Science Communication and Policy Research, New Delhi, India.
Top Curr Chem (Cham). 2022 Feb 5;380(2):10. doi: 10.1007/s41061-022-00365-x.
The present review article strives to compile the latest synthetic approaches for the synthesis of triazolothiadiazine and its derivatives, along with their diverse pharmacological activities, viz. anticancer, antimicrobial, analgesic and anti-inflammatory, antioxidant, antiviral, enzyme inhibitors (carbonic anhydrase inhibitors, cholinesterase inhibitors, alkaline phosphatase inhibitors, anti-lipase activity, and aromatase inhibitors) and antitubercular agents. The review focuses particularly on the structure-activity relationship of biologically important 1,2,4-triazolo[3,4-b][1,3,4]thiadiazines, which have profound importance in drug design, discovery and development. In silico pharmacokinetic and molecular modeling studies have also been summarized. It is hoped that this review article will be of help to researchers engaged in the development of new biologically active entities for the rational design and development of new target-oriented 1,2,4-triazolo[3,4-b][1,3,4]thiadiazine-based drugs for the treatment of multifunctional diseases.
本文综述了合成三唑并噻二嗪及其衍生物的最新方法，以及它们在多种药理学活性方面的应用，如抗癌、抗菌、镇痛和抗炎、抗氧化、抗病毒、酶抑制剂（碳酸酐酶抑制剂、胆碱酯酶抑制剂、碱性磷酸酶抑制剂、抗脂肪酶活性和芳香酶抑制剂）和抗结核药物。本文特别关注具有重要生物学意义的 1,2,4-三唑并[3,4-b][1,3,4]噻二嗪的构效关系，这对于药物设计、发现和开发具有深远意义。本文还总结了基于计算机的药代动力学和分子建模研究。希望本文能为从事新型生物活性实体开发的研究人员提供帮助，以合理设计和开发新型以 1,2,4-三唑并[3,4-b][1,3,4]噻二嗪为基础的靶向药物，用于治疗多功能疾病。
