CLARK RF, MA Z, WANG S, NILIUS AM, CHU DT, ZHANG X, OR YD; Interscience Conference on Antimicrobial Agents and Chemotherapy (41st : 2001 : Chicago, Ill.).
Abstr Intersci Conf Antimicrob Agents Chemother Intersci Conf Antimicrob Agents Chemother. 2001 Dec 16-19; 41: abstract no. F-1171.
Abbott Laboratories, Abbott Park, IL
In line with our objective to develop new macrolides that effectively address the growing problem of antimicrobial resistance, we have been pursuing a design strategy which utilizes the 6-O-position of the ketolide core structure as a point of attachment for key aromatic substituents. Recent efforts have focused on optimization of the 6-O-side chain spacer tethering the aromatic residue to the macrolide skeleton. To this end, a series of analogues incorporating a a variety of functionality in the 6-O-side chain were synthesized and evaluated for antibacterial activity. The propargyl spacer group was superior to other side chain modifications investigated. A-217213 is a novel 6-O-substituted ketolide with a quinolinyl group attached to the 6-O-position through a propargylic spacer chain. [figure: see text] This compound possesses excellent antibacterial activity against all major respiratory tract pathogens including macrolide-resistant streptococci.
Publication Types:
Keywords:
- Anti-Bacterial Agents
- Macrolides
- Pharmaceutical Preparations
- Streptococcus
- Structure-Activity Relationship
Other ID:
UI: 102270005
From Meeting Abstracts