Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
Bioorg Med Chem Lett
; 16(5): 1272-6, 2006 Mar 01.
Article
in En
| MEDLINE
| ID: mdl-16337791
ABSTRACT
This report describes 9H-isothiazolo[5,4-b]quinoline-3,4-diones (ITQs) containing aromatic groups at the 7-position that were prepared using palladium-catalyzed cross-coupling and tested against a panel of susceptible and resistant bacteria. In general, these compounds were more effective against Gram-positive than Gram-negative organisms. Many of the ITQs were more potent than contemporary quinolones and displayed a particularly strong antistaphylococcal activity against a clinically important, multi-drug-resistant strain. In contrast with ITQs reported previously, several of the analogues described in this Letter demonstrated low cytotoxic activity against a human cell line.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Quinolines
/
Sulfhydryl Compounds
/
Azo Compounds
/
Hydrocarbons, Aromatic
/
Anti-Bacterial Agents
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2006
Document type:
Article
Affiliation country:
United States