Late-Stage Functionalization of Platensimycin Leading to Multiple Analogues with Improved Antibacterial Activity in Vitro and in Vivo.
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DOI: 10.1021/acs.jmedchem.9b00616
Abstract: Bacterial fatty acid synthases are promising antibacterial targets against multidrug-resistant pathogens. Platensimycin (PTM) is a potent FabB/FabF inhibitor, while its poor pharmacokinetics hampers the clinical development. In this study, a focused library of PTM derivatives… read more here.
Keywords: late stage; functionalization platensimycin; antibacterial activity; stage functionalization ... See more keywords