Compounds containing oxathiadiazolone nucleus bearing substituted coumarin ring were designed and synthesized while retaining the pharmacophores required for binding with p38 MAP kinase. A four-step synthetic scheme was employed for the synthesis of 7-methoxy-4-(3t?-substituted-2t?-oxo-1t?,2t?,3t?,5t?-oxathiadiazol-4t?-yl)-coumarin. The reactions were monitored by TLC and structures of the intermediates and the target compounds were ascertained by IR, NMR, Mass spectral data. The compounds were found to possess anti-inflammatory activity comparable to indomethacin. Superimposition studies of the target compounds with the lead p38 kinase inhibitors suggested that anti-inflammatory activity of the target compounds may be due to p38 MAP kinase inhibition. It was also suggested that methoxy group on coumarin nucleus may improve the binding profile with p38 MAP kinase.

中文翻译：

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可能通过p38 MAP激酶抑制作用具有抗炎活性的香豆素取代的草二恶唑酮衍生物的设计与合成

设计并合成了含有带有取代的香豆素环的恶二恶唑酮核的化合物，同时保留了与p38 MAP激酶结合所需的药效团。采用四步合成方案合成7-甲氧基-4-（3t′-取代的-2t′-氧代-1t′，2t′，3t′，5t′-氧杂二唑-4t′-基）-香豆素。 。通过TLC监测反应，并且通过IR，NMR，质谱数据确定中间体和目标化合物的结构。发现该化合物具有与消炎痛相当的抗炎活性。目标化合物与先导性p38激酶抑制剂的叠加研究表明，目标化合物的抗炎活性可能归因于p38 MAP激酶的抑制作用。