Helena I M Boshoff, Katherine Young, Yong-Mo Ahn, Veena D Yadav, Brendan M Crowley, Lihu Yang, Jing Su, Sangmi Oh, Kriti Arora, Jenna Andrews, Michelle Manikkam, Michelle Sutphin, Anthony J Smith, Danielle M Weiner, Michaela K Piazza, Joel D Fleegle, Felipe Gomez, Emmannual K Dayao, Brendan Prideaux, Matthew Zimmerman, Firat Kaya, Jansy Sarathy, Vee Yang Tan, Laura E Via, Richard Tschirret-Guth, Anne J Lenaerts, Gregory T Robertson, Véronique Dartois, David B Olsen, Clifton E Barry
Linezolid is a drug with proven human antitubercular activity whose use is limited to highly drug-resistant patients because of its toxicity. This toxicity is related to its mechanism of action─linezolid inhibits protein synthesis in both bacteria and eukaryotic mitochondria. A highly selective and potent series of oxazolidinones, bearing a 5-aminomethyl moiety (in place of the typical 5-acetamidomethyl moiety of linezolid), was identified. Linezolid-resistant mutants were cross-resistant to these molecules but not vice versa...
April 6, 2024: ACS Infectious Diseases