A series of novel 6-(aminomethylphenoxy)benzoxaborole analogs was synthesized for the investigation of the structure-activity relationship of the inhibition of TNF-alpha, IL-1beta, and IL-6, from lipopolysaccharide stimulated peripheral blood mononuclear cells. Compounds 9d and 9e showed potent activity against all three cytokines with IC50 values between 33 and 83nM. Chloro substituted analog 9e (AN3485) is considered to be a promising lead for novel anti-inflammatory agent with a favorable pharmacokinetic profile.
Anne Wu合作论文数1Rashmi Sharma合作论文数1Chen Dong合作论文数1Plattner J合作论文数1Virtucio Charlotte合作论文数1Yongkang Zhang合作论文数School of Materials Science and Engineering, Xiangtan University1
Kurt Jarnagin合作论文数Hormone Research Laboratory Institute, University of California San Francisco1Tsutomu Akama合作论文数Anacor Pharmaceuticals, Inc.1
Xiaoqing Fan合作论文数1Richard H. Kimura合作论文数1
Rajeshwar Singh合作论文数NAEJA Pharmaceutical Inc.1Yvonne Freund合作论文数1
James A. Nieman合作论文数Department of Chemistry, University of Calgary1Xiaosong Lu合作论文数1
