OBOC screening of high activity and low-toxic polymyxin analogs against MCR-1 resistant strains.

We performed inverse synthesis to create 1152 structural analogs of polymyxin B with modified hydrophilicity and charge properties using OBOC technology. This led to the identification of two promising candidates that provided insights into structure-activity relationships. These compounds maintained high antibacterial activity while expanding the safety window 4-16 times.