<br/>A well-known threat to public health is bacterial resistance to current antibiotics. Unfortunately, the growing burden of antibiotic resistance is coupled by reduced efforts in producing new antibiotics, underlining the need for research dedicated to the development of novel drugs. A lesser-known public health threat exists in Neglected Tropical Diseases (NTDs), a category of parasitic diseases that include malaria, sleeping sickness, chagas disease, and leishmaniasis. While NTDs are quite abundant, they predominantly affect communities that have little access to proper treatment leading to reduced efforts in producing novel anti-parasitic drugs. Thus, research grounded in academia plays a crucial role in helping to combat the existing limitations and the development of resistance against antibiotics and NTDs treatments.<br/> <br/>Peptide natural products have attracted considerable synthetic interest due to their broad spectrum of activity. Xenortides, a tripeptide natural product, have shown both antimicrobial and anti-parasitic activity making their derivatives a promising synthetic target for potential use as both an antibiotic and an NTD treatment. Peptide natural products lend themselves to broad structure-activity relationship (SAR) studies due to the commercial availability of their amino acids precursors. The central hypothesis of this research is to synthesize, characterize, and biologically evaluate derivatives of xenortide natural products with SAR studies. Work done on these derivatives will potentially lead to the identification of a promising antibacterial and anti-parasitic drug for further biological testing.

Synthesis and biological evaluation of xenortide derivatives

255th National Meeting (2018)

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