drug-resistant pathogens. We report the first total synthesis of laspartomycin C as well as a series of structural variants. Laspartomycin C was found to specifically bind undecaprenyl phosphate (C55-P) and inhibit formation of the bacterial cell wall precursor lipid II. While several clinically used antibiotics target the lipid II pathway, there are no approved drugs that act on its C55-P precursor.
Laspartomycin C是脂肽抗生素,对多种革兰氏阳性细菌(包括耐药性病原体)具有活性。我们报告了拉丝霉素C以及一系列结构变体的第一个全合成。发现Laspartomycin C特异性结合
十一碳烯基
磷酸酯(C 55 -P)并抑制细菌细胞壁前体脂质II的形成。尽管几种临床使用的抗生素靶向脂质II途径,但尚无批准的药物可作用于其C 55 -P前体。