Semisynthesis of Arsinothricin and Derivatives – 2020-031

The dramatic increase in bacterial resistance toantibiotics is a grave threat to global health. A dearth of new antibiotics hasfostered the emergence and worldwide spread of multidrug resistant (MDR)bacteria, resulting in an increase of serious infections with high mortalityrates. To overcome this serious health concern, discovery and development ofnew antibiotics are urgently needed. Arsinothricin[2-amino-4-(hydroxymethylarsinoyl)-butanoic acid or AST] has broad spectrumantibiotic activity and is effective against both Gram-positive andGram-negative bacteria, including carbapenem-resistant Enterobacter cloacae (CRE), one of the World Health Organization criticalpriority pathogens,and Mycobacterium bovis BCG, acausative agent of animal tuberculosis that is closely related to the humanpathogen MTB. AST is produced by the rice rhizospherebacterium Burkholderia gladioli GSRB05. However, the amounts of ASTproduced by such bacterium are insufficient for further biochemical andclinical characterization of this antibiotic and for development of moreeffective derivatives. Overcoming this obstacle requires a chemical syntheticprocess. FIU inventors have developed methods for the semi-synthesis of the antibiotic AST and derivatives.These methods comprise steps for synthesizing the precursor of AST, hydroxyarsinothricin [2-amino-4-(dihydroxyarsonoyl)butanoicacid orAST-OH], and steps of convertingAST-OH to AST through an enzymatic methylation of AST-OH. Advantageously, it is anticipated that both the chemical synthesis andenzymatic methylation can be scaled up to produce ASTand its derivatives in amounts sufficient for further drug development. Anne Laure Schmitt Olivier aschmitt@fiu.edu 305-348-5948

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