Boron-Containing Analogs of Fosmidomycin: Benzoxaborole Derivatives Exhibit Promising Activity Against Resistant Pathogens.

ABSTRACT: The rise of antimicrobial resistance presents an urgent challenge that necessitates the development of novel therapeutic agents with distinct mechanisms of action. This research explores boron-containing compounds as potential neutral phosphate/phosphonate isosteres of fosmidomycin, a potent inhibitor of 1-deoxy-d-xylulose-5-phosphate reductoisomerase (IspC) within the nonmevalonate isoprenoid biosynthesis (MEP) pathway, with limited clinical utility due to poor pharmacokinetics. We report the synthesis of a library of 15 boron-containing analogs of fosmidomycin and their comprehensive evaluation as IspC inhibitors and antimicrobial agents. The compounds did not demonstrate significant activity against the intended IspC target, thus providing evidence that these boron moieties may have lim

SUBMITTER: Gamrat JM 

PROVIDER: S-EPMC12311745 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature