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Updated: Dec 11, 2025

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Semisynthesis of the Organoarsenical Antibiotic Arsinothricin
Sazzad H Suzol1, A Hasan Howlader1, Adriana E Galván2
1Department of Chemistry and Biochemistry, Florida International University, Miami, Florida 33199, United States.
Abstract:
Arsinothricin [AST (1)], a new broad-spectrum organoarsenical antibiotic, is a nonproteinogenic analogue of glutamate that effectively inhibits glutamine synthetase. We report the chemical synthesis of an intermediate in the pathway to 1, hydroxyarsinothricin [AST-OH (2)], which can be converted to 1 by enzymatic methylation catalyzed by the ArsM As(III) S-adenosylmethionine methyltransferase. This is the first report of semisynthesis of 1, providing a source of this novel antibiotic that will be required for future clinical trials.
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