A Unified Approach to Synthesizing Four Linezolid Metabolites That May Cause Thrombocytopenia.

ABSTRACT: Background/Objectives: Linezolid is a first-in-class oxazolidinone antibiotic that exhibits activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci. However, its clinical use is often restricted because of hematological toxicities, particularly thrombocytopenia, in patients with renal impairment. That side effect is thought to result from the systemic accumulation of pharmacologically inactive metabolites generated by oxidative degradation and ring-opening of the morpholine, but the details remain unclear. In this study, we established a novel synthetic route for four linezolid metabolites (PNU-142618, 142300, 142586 and 173558). Methods: The four major metabolites, which are secondary or tert

SUBMITTER: Oikawa N 

PROVIDER: S-EPMC12735765 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature