Topics in Current Chemistry ( IF 7.1 ) Pub Date : 2022-02-05 , DOI: 10.1007/s41061-022-00365-x Ranjana Aggarwal 1, 2 , Mona Hooda 1 , Prince Kumar 1 , Garima Sumran 3
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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.
Graphical Abstract
中文翻译：
1,2,4-三唑并[3,4-b][1,3,4]噻二嗪支架的合成和药用方面的愿景
本综述文章力求汇编合成三唑并噻二嗪及其衍生物的最新合成方法，以及它们不同的药理活性，即。抗癌剂、抗菌剂、镇痛剂和抗炎剂、抗氧化剂、抗病毒剂、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）和抗结核剂。该综述特别关注具有重要生物学意义的 1,2,4-三唑[3,4- b][1,3,4]噻二嗪，在药物设计、发现和开发中具有深远的意义。还总结了计算机药代动力学和分子模型研究。希望这篇综述文章能够对从事新型生物活性实体开发的研究人员有所帮助，以合理设计和开发新的靶向1,2,4-三唑并[3,4- b ][1, 3,4]噻二嗪类药物治疗多功能疾病。
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