Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
Wiles JA,
Song Y,
Wang Q,
Lucien E,
Hashimoto A,
Cheng J,
Marlor CW,
Ou Y,
Podos SD,
Thanassi JA,
Thoma CL,
Deshpande M,
Pucci MJ,
Bradbury BJ.
Achillion Pharmaceuticals, Inc., 300 George Street, New Haven, CT 06511-6653, USA. jwiles@achillion.com
We synthesized a diverse series of 9H-isothiazolo[5,4-b]quinoline-3,4-diones containing heteroaromatic groups at the 7-position via palladium-catalyzed cross-coupling. Many of these compounds demonstrated potent antistaphylococcal activity (MICs 2 microg/mL) against a multi-drug-resistant strain (ATCC 700699) and low cytotoxic activity (CC(50)>100 microM) against the human cell line Hep2 (laryngeal carcinoma).
PMID: 16337789 [PubMed - indexed for MEDLINE]