Abstract: A compound with broad-spectrum antibacterial activity and its antibacterial composition are provided. The compound with broad-spectrum antibacterial activity has formula (I), which are antibacterial drug source compounds with a broad antibacterial spectrum, good antibacterial activity, suitable in vivo pharmacokinetics, and significant in vivo therapeutic effects. Preferred compound BAB159 has good antibacterial activity against Staphylococcus, Clostridium perfringens, Enterococcus, Bacillus, Streptococcus, Haemophilus, Candida krusei, Aspergillus niger, and Trichophyton, which is comparable or better than the listed drugs. The combination of preferred compound BAB159 and polymyxin E exhibits significantly enhanced synergistic antibacterial activity, especially against multidrug-resistant strains.

Abstract: Use of a C-JUN N-terminal kinase inhibitor, SU3327, in the preparation of a medicament for reducing cytotoxicity and nephrotoxicity of polymyxin, wherein the polymyxin is preferably Polymyxin E. A treatment with a combination of SU3327 and Polymyxin E can significantly inhibit cytotoxicity and nephrotoxicity of Polymyxin E.

Abstract: The present invention provides use of a C-JUN N-terminal kinase inhibitor, SU3327, in the preparation of a medicament for enhancing the efficacy of polymyxin against bacterial infection, and use of a composition of SU3327 and polymyxin in the preparation of a medicament for an enhanced efficacy against bacterial infection, wherein the polymyxin is preferably Polymyxin E. The invention not only shows an enhanced antibacterial activity of polymyxin by SU3327 in synergy through minimum inhibitory concentration tests in checkerboard assays and in vitro bacterial growth curves, but also confirms the ability of SU3327 to enhance polymyxin along with its effectiveness in vivo in the experiments with a model of mice infected with drug resistant bacteria at the animal level. The invention provides a new use of SU3327 in enhancing antibacterial activities of polymyxin antibiotics, resolving the technical problems such as clinical resistance to polymyxin, low clinical therapeutic index of polymyxin, etc.

Abstract: A compound with broad-spectrum antibacterial activity and its antibacterial composition are provided. The compound with broad-spectrum antibacterial activity has formula (I), which are antibacterial drug source compounds with a broad antibacterial spectrum, good antibacterial activity, suitable in vivo pharmacokinetics, and significant in vivo therapeutic effects. Preferred compound BAB159 has good antibacterial activity against Staphylococcus, Clostridium perfringens, Enterococcus, Bacillus, Streptococcus, Haemophilus, Candida krusei, Aspergillus niger, and Trichophyton, which is comparable or better than the listed drugs. The combination of preferred compound BAB159 and polymyxin E exhibits significantly enhanced synergistic antibacterial activity, especially against multidrug-resistant strains.