Abstract:Tuberculosis remains a highly infectious disease across the world. In the identification ofnew antitubercular agents, coumarin clubbed thiadiazole amides have been synthesized and evaluatedfor in vitro antitubercular activity. Owing to the growing concern of chemicals and their impact on theenvironment, greener and faster reaction conditions needed to be incorporated. Therefore, we usedTBTU as a coupling reagent for efficient and facile synthesis of substituted-N-(5-((7-methyl-2-oxo-2Hchromes-4-yl)-methyl)-1,3, 4-thiadiazol-2-yl)-benzamide 4a-j with good yields up to 95% in mild reactionconditions. All the synthesized compounds were evaluated in vitro for anti-tubercular activityagainst the H37Rv strain of M. tuberculosis. Compounds 4c, 4d, and 4f were found active at 12.5μg/mL against M. tb H37Rv. Electron withdrawing substituents present on aromatic side chains showedpromising anti-tubercular activity.

中文翻译：

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使用 TBTU 作为偶联剂合成取代的 -N-(5-((7-Methyl-2-Oxo-2H-Chromen-4-yl)-Methyl)-1,3,4-Thiadiazol-2-yl)-Benzamide 衍生物抗结核活性剂及其评价

摘　要：结核病在世界范围内仍然是一种高度传染性疾病。在鉴定新的抗结核药物中，合成了香豆素棒状噻二唑酰胺，并对其体外抗结核活性进行了评估。由于对化学品及其对环境影响的日益关注，需要纳入更环保、更快速的反应条件。因此，我们使用 TBTU 作为偶联剂，高效简便地合成取代的-N-(5-((7-methyl-2-oxo-2Hchromes-4-yl)-methyl)-1,3, 4-thiadiazol-2 -yl)-苯甲酰胺 4a-j 在温和的反应条件下具有高达 95% 的良好收率。所有合成的化合物都在体外评估了对结核分枝杆菌 H37Rv 菌株的抗结核活性。发现化合物 4c、4d 和 4f 在 12.5μg/mL 时对 M. tb H37Rv 有活性。