Synthesis, microbiological evaluation and structure activity relationship analysis of linezolid analogues with different C5-acylamino substituents

• DOI: 10.1016/j.bmc.2021.116397
• Publication Date: 2021-09-08T08:10:15Z
• Authors: Christos Matsingos; Taha Al-Adhami; Shirin Jamshidi; Charlotte Hind; Melanie Clifford; J. Mark Sutton; Khondaker Miraz R...
• Keywords: Linezolid; Moiety; Structure–activity relationship

Antimicrobial resistance and lack of new antibiotics to treat multidrug-resistant (MDR) bacteria is a significant public health problem. There discovery void the pipeline classes in clinical development almost empty. Therefore, it important understand structure activity relationships (SAR) current chemical as that can help drug community their efforts develop by modifying existing antibiotic classes. We studied SAR C5-acylaminomethyl moiety linezolid, an oxazolidinone antibiotic, synthesizing 25 compounds containing various aromatic, heteroaromatic aliphatic substitutions. Our findings suggest this position highly for function class, since only smaller non-polar fragments are tolerated at while larger polar ones lead decrease compared linezolid. have led us construct relationship, around provides valuable insight into class antibiotics.