2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2006 Mar 1;16(5):1277-81. doi: 10.1016/j.bmcl.2005.11.064.
Jason A Wiles 1,  Yongsheng Song,  Qiuping Wang,  Edlaine Lucien,  Akihiro Hashimoto,  Jijun Cheng,  Christopher W Marlor,  Yangsi Ou,  Steven D Podos,  Jane A Thanassi,  Christy L Thoma,  Milind Deshpande,  Michael J Pucci,  Barton J Bradbury
Affiliations

Affiliation

  • 1 Achillion Pharmaceuticals, Inc., 300 George Street, New Haven, CT 06511-6653, USA. [email protected]
PMID: 16337789 DOI: 10.1016/j.bmcl.2005.11.064
Abstract

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).

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