多元咪唑[2,1-b][1,3]噻嗪类化合物的合成及非甾体抗炎剂的评价

ECSOC-25 Pub Date : 2021-11-14 DOI:10.3390/ecsoc-25-11692
N. Slyvka, S. Holota, L. Saliyeva, M. Vovk
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引用次数: 0

摘要

本工作致力于咪唑[2,1- b][1,3]噻嗪衍生物的合成,作为可能的抗炎药。基于多取代2-氯吡啶与3-羟基咪唑[2,1- b][1,3]噻嗪的相互作用,提出了(2-吡啶基氧基)取代亚胺-偶氮[2,1- b][1,3]噻嗪的合成方法。在上述反应中观察到吡啶环2位选择性亲核取代。合成的(2-吡啶基氧基)取代咪唑[2,1- b][1,3]噻嗪类药物性质在硅片上用SwissADME进行了研究,并进行了卡拉胶体内抗炎活性试验。具有令人满意的类药物和药理特征的hit -化合物被认为是未来结构优化和深入研究的有希望的对象。
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Synthetic Approach to Diversified Imidazo[2,1-b][1,3]thiazines and Its Evaluation as Non-Steroidal Anti-Inflammatory Agents †
: The present work is devoted to the synthesis of imidazo[2,1- b ][1,3]thiazine derivatives as possible anti-inflammatory agents. The synthetic approach to (2-pyridinyloxy)substituted imid-azo[2,1- b ][1,3]thiazines based on the interaction of the polysubstituted 2-chloropyridines with 3-hydroxy-imidazo[2,1- b ][1,3]thiazines was proposed. Selective nucleophilic substitution in position 2 of pyridine ring was observed in the mentioned reaction. The synthesized (2-pyridinyloxy)substi-tuted imidazo[2,1- b ][1,3]thiazines drug-like properties were studied in silico using SwissADME and anti-inflammatory activity in carrageenan test in vivo. Hit-compounds with satisfactory drug-like and pharmacological features were identified as promising objects for futhercoming structure opti-mization and in-depth studies.
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