作为抗菌剂的1,2,3-三唑β-内酰胺共轭物
1,2,3-Triazole β-lactam conjugates as antimicrobial agents.
作者信息
Kaur Rajneesh, Singh Raman, Kumar Antresh, Kaur Satvinder, Priyadarshi Nitesh, Singhal Nitin Kumar, Singh Kuldeep
机构信息
Department of Chemistry, MMEC, Maharishi Markandeshwar (Deemed to be University), Mullana, Haryana, 133207, India.
Department of Biotechnology, Central University of South Bihar, Panchanpur, Gaya, 824236, India.
出版信息
Heliyon. 2020 Jun 27;6(6):e04241. doi: 10.1016/j.heliyon.2020.e04241. eCollection 2020 Jun.
A convenient and efficient synthesis of new triazole β-lactam conjugates using click chemistry is described. β-lactam and were prepared using cycloaddition strategy and propargylated at -1 to afford compounds and . Cu-catalyzed click reaction of these β-lactams and with different aryl azides provided 1,2,3-triazole conjugates and , respectively. The products were fully characterized spectroscopically and tested against Gram-(+) and Gram-(-) bacteria. Compound and were found to be most active.
描述了一种使用点击化学方便高效地合成新型三唑β-内酰胺共轭物的方法。β-内酰胺 使用环加成策略制备，并在-1位进行炔丙基化反应以得到化合物 和 。这些β-内酰胺 与不同芳基叠氮化物的铜催化点击反应分别提供了1,2,3-三唑共轭物 和 。通过光谱对产物进行了全面表征，并针对革兰氏阳性菌和革兰氏阴性菌进行了测试。发现化合物 和 活性最高。
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