Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2003 Dec 1;13(23):4229-33.

Structure-activity relationship in the oxazolidinone-quinolone hybrid series: influence of the central spacer on the antibacterial activity and the mode of action.

Author information

1
Morphochem AG, Schwarzwaldallee 215, CH 4058, Basel, Switzerland. christian.hubschwerlen@morphochem.ch

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.

PMID:
14623007
DOI:
10.1016/j.bmcl.2003.07.028
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center