Instituto Universitario de Bio-Orgánica Antonio González (CIBICAN), Departamento de Química Orgánica, Universidad de La Laguna, Avda. Astrofísico Fco. Sánchez 2, 38206 La Laguna, Tenerife, Spain.
Department of Molecular Biology, The John Paul II Catholic University of Lublin, ul. Konstantynów 1i, 20-708 Lublin, Poland.
Molecules. 2018 Jan 18;23(1):199. doi: 10.3390/molecules23010199.
A new series of coumarin-1,2,3-triazole conjugates with varied alkyl, phenyl and heterocycle moieties at C-4 of the triazole nucleus were synthesized using a copper(I)-catalysed Huisgen 1,3-dipolar cycloaddition reaction of corresponding -propargylated coumarin () or -propargylated coumarin () with alkyl or aryl azides. Based on their minimal inhibitory concentrations (MICs) against selected microorganisms, six out of twenty-six compounds showed significant antibacterial activity towards (MIC = 12.5-50 µg/mL). Moreover, the synthesized triazoles show relatively low toxicity against human erythrocytes.
一系列新型的香豆素-1,2,3-三唑化合物，其中三唑核的 C-4 位上具有不同的烷基、苯基和杂环取代基，是通过相应的 -丙炔基香豆素（）或 -丙炔基香豆素（）与烷基或芳基叠氮化物的铜（I）催化的 Huisgen 1,3-偶极环加成反应合成的。根据它们对选定微生物的最小抑菌浓度（MIC），26 种化合物中有 6 种对表现出显著的抗菌活性（MIC = 12.5-50 µg/mL）。此外，合成的三唑类化合物对人红细胞的毒性相对较低。
