Huigens Robert W, Rogers Steven A, Steinhauer Andrew T, Melander Christian
North Carolina State University Chemistry Department, 2620 Yarborough Drive, Raleigh, North Carolina 27695-8204, United States of America.
Org Biomol Chem. 2009 Feb 21;7(4):794-802. doi: 10.1039/b817926c. Epub 2009 Jan 12.
A chemically diverse library of TAGE-triazole conjugates was synthesized utilizing click chemistry on the TAGE scaffold. This library of small molecules was screened for anti-biofilm activity and found to possess the ability of inhibiting biofilm formation against Acinetobacter baumannii, Staphylococcus aureus and Pseudomonas aeruginosa. One such compound in this library demonstrated the most potent inhibitory effect against Staphylococcus aureus biofilm formation that has been displayed by any 2-aminoimidazole derivative.
利用点击化学在TAGE支架上合成了一个化学性质多样的TAGE-三唑共轭物文库。对这个小分子文库进行了抗生物膜活性筛选,发现它具有抑制鲍曼不动杆菌、金黄色葡萄球菌和铜绿假单胞菌生物膜形成的能力。该文库中的一种此类化合物对金黄色葡萄球菌生物膜形成表现出最有效的抑制作用,这是任何2-氨基咪唑衍生物都未曾表现出的。