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

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.

Graphical abstractA series of borinic acid picolinate esters were synthesized and screened for antibacterial and anti-inflammatory activities. From these studies, we selected 3-hydroxypyridine-2-carbonyloxy-bis(3-chloro-4-methylphenyl)borane (AN0128) as a clinical candidate for dermatological diseases.Figure optionsDownload full-size imageDownload as PowerPoint slide