Synthesis of Antimicrobial Mimetic Peptide Analogs and their Structural Activity Relationship

초록

Natural antimicrobial peptides have great effect against microorganism. The previous research by many research group suggested that backbone modification of peptides with isosteric units resulted in the decrease of biological activity. In this communication, we investigated the effect of backbone modification with reduced amide bond and its structure activity relationship. We choose lysine and leucine rich cationic antimicrobial peptide as model system and subsituted the position 1 and position 7 by reduced amide bonds to investigate not only the secondary structure but also net charge effect. The biological activities associated with antimicrobial assay as well as hemolytic activities, liposome assay and secondary structure was investigated using circular dichroism. Overall study indicated that, the secondary structural change is not only important for maintaining the biological activity but also net charge effect.