Department of Chemistry, North Carolina State University, Raleigh, NC 27695, USA.
Org Biomol Chem. 2012 Apr 7;10(13):2552-61. doi: 10.1039/c2ob06871k. Epub 2012 Feb 2.
An efficient synthetic route to a series of substituted 2-aminopyrimidine (2-AP) derivatives has been developed. Subsequent biofilm screening has allowed comparison between the biological activity of these new derivatives and that of the 2-aminoimidazole class of anti-biofilm compounds. Several derivatives displayed the ability to modulate bacterial biofilm formation, exhibiting greater activity against Gram-positive strains than Gram-negative strains. Additionally some 2-aminopyrmidines were able to suppress MRSA resistance to conventional antibiotics.
已开发出一系列取代的 2-氨基嘧啶（2-AP）衍生物的有效合成路线。随后的生物膜筛选允许比较这些新衍生物和抗生物膜化合物的 2-氨基咪唑类的生物活性。几种衍生物表现出调节细菌生物膜形成的能力，对革兰氏阳性菌株的活性大于革兰氏阴性菌株。此外，一些 2-氨基嘧啶能够抑制 MRSA 对常规抗生素的耐药性。
