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

  • Bioorg Med Chem Lett. 2006 Dec 1;16(23):5963-7. doi: 10.1016/j.bmcl.2006.08.130.
Stephen J Baker " href="affiliation-1" ref="linksrc=author_aff">  #  1 ,  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
Affiliations
  • 1. Anacor Pharmaceuticals, Inc., 1060 E. Meadow Circle, Palo Alto, CA 94303, USA. [email protected]
  • # Contributed equally.
PMID: 16997550 DOI: 10.1016/j.bmcl.2006.08.130
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.

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