Antimicrobial-resistant infectious strains have risen over the past 20 years limiting the lifespans of existing antibiotics. Since the 1940s, the discovery of antibiotics has been rooted in natural product isolation. In the constant search for new chemotherapeutic drugs, natural products are increasingly relied upon due to their diverse pharmaceutical scope and thus attracting considerable synthetic interest. Recent technological advances have enabled the isolation and growth of uncultured bacteria, which have produced previously inaccessible natural products. Among these natural products are the antimicrobial peptides, which have emerged as promising candidates for developing new antibiotics. Since many of the peptide natural products' precursors are commercially available amino acids, peptide natural products are amendable for structure-activity relationship (SAR) studies. Such studies have led to modified natural product derivatives that are effective against resistant strains of bacteria. Therefore, this research focuses on the synthesis of antibacterial peptide derivatives by using a fragment-based approach followed by biological evaluation of each fragment.

Fragment-based synthesis and biological evaluation of antimicrobial peptide derivatives

255th National Meeting (2018)

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