The disclosure provides cationic peptidopolysaccharides of Formula I: which has a bacterial peptidoglycan-mimetic structure, and shows outstanding broad spectrum activities against clinically significant bacteria and fungi. The structural affinity of these compounds with microbial cell wall constituents promotes its passage to the cytoplasmic membrane resulting in excellent antimicrobial activity and record high selectivity. The disclosure also describes methods of making and using cationic peptidopolysaccharides of Formula I.
