TY - JOUR
T1 - Synthesis and antimicrobial evaluation of 3-methanone-6-substituted- benzofuran derivatives
AU - Liu, Jingbao
AU - Jiang, Faqin
AU - Jiang, Xizhen
AU - Zhang, Wei
AU - Liu, Jingjing
AU - Liu, Wenlu
AU - Fu, Lei
N1 - Funding Information:
We thank the National Comprehensive Technology Platforms for Innovative Drug R&D ( 2009ZX09301-007 ) and Special Research Fund to Doctoral Program of College and University ( 20110073120081 ) for the financial support. We thank Professor Xiaobo Li's Laboratory (Shanghai Jiao Tong University) for the biological support of this research.
PY - 2012/8
Y1 - 2012/8
N2 - Seventeen benzofuran derivatives were synthesized and screened for their antibacterial activities against Escherichia coli, Staphylococcus aureus, Methicillin-resistant S. aureus, Bacillus subtilis, and Pseudomonas aeruginosa. Seven of them have showed excellent antibacterial activities compared to the positive controls (Cefotaxime and Sodium Penicillin). The substitutions at C-6 and C-3 positions of these derivatives were found to greatly impact on the antibacterial activity and strains specificity, respectively. Specifically, compounds bearing a hydroxyl group at C-6 (5a, 5b, 5c and 12) offered excellent antibacterial activities against all five above-mentioned strains (MIC 80 = 0.78-12.5 ug/mL), and those with imine (15) and (3, 4, 5-trimethoxyphenyl) methanone (7e), respectively, at C-3 position showed selective activity against S. aureus among five tested strains with great MIC80 values (3.12-12.5 ug/mL).
AB - Seventeen benzofuran derivatives were synthesized and screened for their antibacterial activities against Escherichia coli, Staphylococcus aureus, Methicillin-resistant S. aureus, Bacillus subtilis, and Pseudomonas aeruginosa. Seven of them have showed excellent antibacterial activities compared to the positive controls (Cefotaxime and Sodium Penicillin). The substitutions at C-6 and C-3 positions of these derivatives were found to greatly impact on the antibacterial activity and strains specificity, respectively. Specifically, compounds bearing a hydroxyl group at C-6 (5a, 5b, 5c and 12) offered excellent antibacterial activities against all five above-mentioned strains (MIC 80 = 0.78-12.5 ug/mL), and those with imine (15) and (3, 4, 5-trimethoxyphenyl) methanone (7e), respectively, at C-3 position showed selective activity against S. aureus among five tested strains with great MIC80 values (3.12-12.5 ug/mL).
KW - Antimicrobial
KW - Benzofuran
KW - Synthesis
UR - http://www.scopus.com/inward/record.url?scp=84864405534&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2012.05.013
DO - 10.1016/j.ejmech.2012.05.013
M3 - Article
C2 - 22673144
AN - SCOPUS:84864405534
SN - 0223-5234
VL - 54
SP - 879
EP - 886
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -