The present invention pertains to the combinatorial synthesis of antibacterial agents that inhibit the Mur-pathway enzymes involved in bacterial cell wall assembly. The method uses p-alkoxybenzylidene as the linker for the attachment of a derivatized muramic acid to the polymeric resin support. This intermediate becomes the starting point for the combinatorial synthesis, which in conjunction with split-pooling techniques allows rapid synthesis of diverse analogues for high-throughput screening (HTS). The invention is further directed to the libraries of these finished compounds that vary at the peptide, N-acyl and anomeric UDP positions.
本发明涉及抑制参与细菌细胞壁组装的缪拉途径酶的抗菌剂的组合合成。该方法使用对烷氧基亚苄基作为连接剂,将衍生化的缪拉酸连接到聚合物
树脂载体上。这种中间体成为组合合成的起点,与分池技术相结合,可快速合成用于高通量筛选(H
TS)的各种类似物。本发明进一步涉及这些在肽、N-酰基和同分异构体
UDP 位置上不同的成品化合物库。