HOU Y, QIU Y, VO NH, JIAN T, BUSUYEK M, HALEY T, POLEMEROPOULOS A, PHAN LT, OR YS; Interscience Conference on Antimicrobial Agents and Chemotherapy (43rd: 2003: Chicago, Ill.).

Abstr Intersci Conf Antimicrob Agents Chemother Intersci Conf Antimicrob Agents Chemother. 2003 Sep 14-17; 43: abstract no. F-1187.

Enanta Pharmaceuticals, Inc., Watertown, MA.

BACKGROUND: Broad spectrum antibacterial macrolides with strong activity against H. influenzae are highly sought after in macrolide research. Antibacterial activities of modified 14-membered ring erythromycin antibiotics such as telithromycin and cethromycin (ABT-773), although highly active against a broad range of Gram-positive bacteria, are relatively less active against H. influenzae ( MIC: 1-2 microg/mL). METHODS: Minimal inhibitory concentration (MIC) was determined utilizing the broth-microdilution method as per NCCLS standards. The synthesis and biological activities of these novel 23-O derivatives of OMT will be presented. RESULTS: Typical MICs are in the range of: 0.5-2 microg/mL for H. influenzae; 0.13-2 microg/mL for S. aureus, Ery-S; and 0.06-4 microg/mL for S. pneumoniae Ery-R-mef and S. pyogenes, Ery-R-mef (as compared to 4, 0.5, 8 and 16 microg/mL respectively for erythromycin A). [table: see text] CONCLUSIONS: Modifications of OMT (5-O-Mycaminosyl Tylonolide) at the 23-O position provide novel compounds that show enhanced antibacterial properties against H. influenzae as well as overcoming macrolide resistant bacteria.

Publication Types:

• Meeting Abstracts

Keywords:

• Anti-Bacterial Agents
• Erythromycin
• Haemophilus influenzae
• Ketolides
• Macrolides
• Microbial Sensitivity Tests
• cethromycin
• telithromycin

Other ID:

• GWAIDS0025837

UI: 102265461

From Meeting Abstracts