Cyclic peptides have gained a significant attention in medicinal chemistry and over 50 cyclic peptides currently in clinical use as antibiotics, antifungals, anticancer, and immunosuppressants. In this study, we present the design and antibacterial activities of novel macolacin derivatives with modified side chains. Among them, compound ZM806 exhibited the best antibacterial activities against both sensitive-K. pneumoniae and resistant clinical isolated K. pneumoniae with the MIC of 8 ug/mL, respectively. The result demonstrated that macolacin could serve as a novel molecule for further antibiotic development against Gram-negative bacterial infections.
Yao et al. (Wed,) studied this question.