The present application belongs to the technical field of pharmaceutical
chemistry, and particularly relates to an antibacterial small-molecule compound targeting bacterial
phospholipid synthetase. The present application provides an antibacterial intervention strategy based on a novel
mechanism of action, taking the key
enzyme PlsY of bacterial specific membrane
phospholipid synthesis as a target, and
cracking the cross-resistance problem caused by the concentration of existing
antibacterial drug targets. The
lead compound T1 obtained by screening has strong inhibitory activity on PlsY, can effectively inhibit
pathogenic bacteria such as
Streptococcus pneumoniae and
Staphylococcus aureus, and has better selective
toxicity because the
human body has no PlsY homologous
protein. The compound has a novel structure and can be optimized, and can be rationally designed through structure-activity relationship, and also has
inhibitory effect on
plant pathogenic bacteria. The present application opens up a new antibacterial pathway, provides differentiated candidate molecules and reserves for coping with multi-
drug resistant infections, and has medical and agricultural potential, and has significant innovation and practicality.