2022
DOI: 10.26434/chemrxiv-2022-dm96r
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Total Synthesis of Pargamicin A

Abstract: We report the total synthesis and configurational assignment of pargamicin A, a highly oxidized non-ribosomal peptide that potently inhibits the growth of drug-resistant bacteria. Our synthetic approach relies on late-stage piperazine ring formation and careful selection of condensation reagents to assemble the densely substituted hexapeptide backbone. This work enables the synthesis of pargamicin congeners for the development of structure-activity relationships and informs strategies to access other stericall… Show more

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“…Despite their promising anti-MRSA/VRE activity, there remains no reported chemical synthesis of a member of the pargamicin family . Our goal was to develop an approach amenable to SAR studies through residue substitution.…”
mentioning
confidence: 99%
“…Despite their promising anti-MRSA/VRE activity, there remains no reported chemical synthesis of a member of the pargamicin family . Our goal was to develop an approach amenable to SAR studies through residue substitution.…”
mentioning
confidence: 99%