title: Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.
abstract: Oxazolidinone-quinolone hybrids, which combine the pharmacophores of a quinolone and an oxazolidinone, were synthesised and shown to be active against a variety of susceptible and resistant Gram-positive and Gram-negative bacteria. The nature of the spacer greatly influences the antibacterial activity by directing the mode of action, that is quinolone- and/or oxazolidinone-like activity. The best compounds in this series have a balanced dual mode of action and overcome all types of resistance, including resistance to quinolones and linezolid, in clinically relevant Gram-positive pathogens.
authors: Morphochem AG, Schwarzwaldallee 215, CH 4058, Basel, Switzerland. christian.hubschwerlen@morphochem.ch
authors: Christian
authors: C
authors: Hubschwerlen
authors: Jean-Luc
authors: JL
authors: Specklin
authors: Daniel K
authors: DK
authors: Baeschlin
authors: Yves
authors: Y
authors: Borer
authors: Sascha
authors: S
authors: Haefeli
authors: Christine
authors: C
authors: Sigwalt
authors: Susanne
authors: S
authors: Schroeder
authors: Hans H
authors: HH
authors: Locher
mesh_terms: D000081:Acetamides / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D027101:DNA Topoisomerase IV / Q000037:antagonists & inhibitors; D024881:Drug Resistance, Bacterial; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D000069349:Linezolid; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000081:Acetamides; D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D015363:Quinolones; D027101:DNA Topoisomerase IV; D000069349:Linezolid