Identification of a novel boron-containing antibacterial agent (AN0128) with anti-inflammatory activity, for the potential treatment of cutaneous diseases

Stephen J. Baker, Tsutomu Akama, Yong Kang Zhang, Vittorio Sauro, Chetan Pandit, Rajeshwar Singh, Maureen Kully, Jehangir Khan, Jacob J. Plattner, Stephen J. Benkovic, Ving Lee, Kirk R. Maples

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Abstract

A series of borinic acid picolinate esters were synthesized and screened for their minimum inhibitory concentration (MIC) against Gram-positive and -negative bacteria. Our lead compounds were then screened for anti-inflammatory activity. From these studies, we identified 3-hydroxypyridine-2-carbonyloxy-bis(3-chloro-4-methylphenyl)borane (2g, AN0128) as having the best combination of anti-bacterial and anti-inflammatory activities. This compound is now in clinical development for dermatological conditions.

Original languageEnglish (US)
Pages (from-to)5963-5967
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number23
DOIs
StatePublished - Dec 1 2006

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All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Baker, S. J., Akama, T., Zhang, Y. K., Sauro, V., Pandit, C., Singh, R., Kully, M., Khan, J., Plattner, J. J., Benkovic, S. J., Lee, V., & Maples, K. R. (2006). Identification of a novel boron-containing antibacterial agent (AN0128) with anti-inflammatory activity, for the potential treatment of cutaneous diseases. Bioorganic and Medicinal Chemistry Letters, 16(23), 5963-5967. https://doi.org/10.1016/j.bmcl.2006.08.130