Author/Authors :
Stephen J. Baker، نويسنده , , Tsutomu Akama، نويسنده , , Yong-Kang Zhang، نويسنده , , Vittorio Sauro، نويسنده , , Chetan Pandit، نويسنده , , Rajeshwar Singh، نويسنده , , Maureen Kully، نويسنده , , Jehangir Khan، نويسنده , , Jacob J. Plattner، نويسنده , , Stephen J. Benkovic، نويسنده , , Ving Lee، نويسنده , , Kirk R. Maples، نويسنده ,
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.
Keywords :
structure–activity relationship , atopic dermatitis , Antibacterial activity , Borinic acid picolinate ester
