With the increasing incidence of antibiotic resistance, there is an urgent need to develop new antibiotics with excellent activity against drug-resistant bacteria. Three novel series of tylosin semisynthetic derivatives were designed, synthesized and evaluated for their antibacterial activities against various Gram-positive and Gram-negative bacteria. Among these derivatives, compound C-2 demonstrated potent antibacterial activity against both gram-positive and gram negative bacteria, and non mutagenic. More importantly, compound C-2 displayed high antimicrobial potency against Gram-positive bacteria in a murine model, and was found to be more efficient than tildipirosin. Thus, compound C-2 had great potential as a promising lead compound for the treatment of bacterial infection.

随着抗生素耐药性的增加，迫切需要开发对耐药菌具有优异活性的新型抗生素。设计、合成了三个新型泰乐菌素半合成衍生物系列，并评估了它们对各种革兰氏阳性和革兰氏阴性细菌的抗菌活性。在这些衍生物中，化合物C-2对革兰氏阳性菌和革兰氏阴性菌均表现出有效的抗菌活性，且无致突变性。更重要的是，化合物C-2在小鼠模型中显示出对革兰氏阳性菌的高效抗菌效力，并且被发现比替地匹罗星更有效。因此，化合物C-2作为治疗细菌感染的有前途的先导化合物具有巨大的潜力。