KUBO A, PRESS B, LUEHR GW, GORDEEV MF, TRIAS J; Interscience Conference on Antimicrobial Agents and Chemotherapy (42nd : 2002 : San Diego, Calif.).
Abstr Intersci Conf Antimicrob Agents Chemother Intersci Conf Antimicrob Agents Chemother. 2002 Sep 27-30; 42: abstract no. F-1322.
Versicor, Fremont, CA
Chlamydia species are an important group of obligate intracellular pathogens which causes serious infections, including respiratory tract, ocular, and urogenital infections. Linezolid, an oxazolidinone, is active against C. pneumoniae (MIC range = 1->32 microg/ml), while activity against C. trachomatishas yet to be reported. The anti-chlamydial activity of a series of novel 4'-substituted oxazolidinones against C. trachomatis (ATCC VR-902B) and C. pneumoniae (ATCC VR-1355) was evaluated using a microtiter broth dilution method where inclusions were counted in cyclohexamide-treated HEp-2 and HeLa cell lines. Most compounds displayed better activity (MIC range = 0.25 microg/ml - 8 microg/ml) than linezolid (MIC = 4 microg/ml) against C. pneumoniae. Several compounds were active against C. trachomatis (MIC range = 1 - >16 microg/ml, linezolid MIC = 1 - 2 microg/ml). SAR for 3-phenyloxazolidinones suggests a good tolerance of structurally different 4'-substituents. In particular, 4'-amido, 4'-acylamino, and 4'-methylsufinyl oxazolidinones were among the most potent compounds. VRC-3125 and VRC-3783 were highly active against C. pneumoniae (MICs = 0.25 and 2 microg/ml) and C. trachomatis (MICs = 0.25 and 1 microg/ml), and displayed good antibacterial activity against other key pathogens such as S. pneumoniae (MIC = 0.5 microg/ml) and S. aureus (MIC = 1 microg/ml). [figure: see text] The discovery of novel oxazolidinones with activity against Chlamydia species is of potential clinical interest.
Publication Types:
Keywords:
- Acetamides
- Anti-Bacterial Agents
- Chlamydia
- Chlamydia trachomatis
- In Vitro
- Microbial Sensitivity Tests
- Oxazolidinones
- linezolid
Other ID:
UI: 102267747
From Meeting Abstracts