Department of Chemistry, North Carolina State University, Raleigh, NC 27695-8024, USA.
Eur J Med Chem. 2013 Apr;62:59-70. doi: 10.1016/j.ejmech.2012.12.005. Epub 2012 Dec 20.
The pyrrole-imidazole alkaloids are a 2-aminoimidazoles containing family of natural products that possess anti-biofilm activity. A library of 1,4-di-substituted 2-aminoimidazole/triazoles (2-AITs) was synthesized, and its anti-biofilm activity as well as oxacillin resensitization efficacy toward methicillin resistant Staphylococcus aureus (MRSA) was investigated. These 2-AITs were found to inhibit biofilm formation by MRSA with low micromolar IC50 values. Additionally, the most active compound acted synergistically with oxacillin against MRSA lowering the minimum inhibitory concentration (MIC) 4-fold.
吡咯并咪唑生物碱是一类含有 2-氨基咪唑的天然产物，具有抗生物膜活性。合成了一系列 1,4-二取代 2-氨基咪唑/三唑（2-AITs），并研究了它们对耐甲氧西林金黄色葡萄球菌（MRSA）的抗生物膜活性和对苯唑西林的再敏化作用。这些 2-AITs 以低微摩尔的 IC50 值抑制 MRSA 的生物膜形成。此外，最有效的化合物与苯唑西林对 MRSA 表现出协同作用，使最低抑菌浓度（MIC）降低了 4 倍。
