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

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Baker SJ, Akama T, Zhang YK, Sauro V, Pandit C, Singh R, Kully M, Khan J, Plattner JJ, Benkovic SJ, Lee V, Maples KR

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. Epub 2006 Sep 25.

PubMed ID
16997550 [ View in PubMed
]
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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