2. Academic Validation
  3. 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

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. 2006 Mar 1;16(5):1272-6. doi: 10.1016/j.bmcl.2005.11.065.
Jason A Wiles 1,  Qiuping Wang,  Edlaine Lucien,  Akihiro Hashimoto,  Yongsheng Song,  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: 16337791 DOI: 10.1016/j.bmcl.2005.11.065
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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