A series of novel 1H-pyrrolo[2,3-d]pyrimidine-1,2,3-triazole derivatives have been synthesized in good to excellent yields. Through the copper-catalyzed azide-alkyne cycloaddition via reaction of 7-(prop-2-ynyl)-7H-pyrrolo[2,3-d]pyrimidine and aryl, heteroaryl and alkyl azides in the presence of CuSO₄·5H₂O and sodium ascorbate. These compounds were evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv strain. Most of these pyrrolopyrimidine-triazole hybrids exhibited good anti tubercular activity. The antimycobacterial assay results showed that the minimum inhibitory concentration of compounds 4q and 4r were 0.78 µg/mL. The molecular docking results also had shown highest Moldock score for same compounds. These novel compounds exhibited good inhibition activities and further structure-activity studies of the derivatives had shown promising features to use in antitubercular therapy.

已经合成了一系列新颖的1 H-吡咯并[2,3 - d ]嘧啶-1,2,3-三唑衍生物。通过铜催化的叠氮化物-炔烃环加成反应，在CuSO ₄ ·5H ₂存在下，由7-（丙-2-炔基）-7 H-吡咯并[2,3- d ]嘧啶与芳基，杂芳基和烷基叠氮化物反应O和抗坏血酸钠。评估了这些化合物对结核分枝杆菌的体外抗分枝杆菌活性H37Rv株。这些吡咯并嘧啶-三唑杂种大多数表现出良好的抗结核活性。抗分枝杆菌检测结果表明，化合物4q和4r的最低抑菌浓度为0.78 µg / mL。分子对接结果也显示出相同化合物的摩尔多克分数最高。这些新颖的化合物表现出良好的抑制活性，对衍生物的进一步结构活性研究表明其可用于抗结核治疗中。