1. Synthesis and biological evaluation of 1,2,4,5-tetrasubstituted imidazoles.
- Author
-
Fang, Yue, Yuan, Rui, Ge, Wen-hui, Wang, Yuan-jiang, Liu, Gui-xiang, Li, Ming-qi, Xu, Jiang-biao, Wan, Yu, Zhou, Sheng-liang, Han, Xi-guang, Zhang, Peng, Liu, Jin-juan, and Wu, Hui
- Subjects
- *
IMIDAZOLES , *CHEMICAL synthesis , *AROMATIC aldehydes , *AMINES , *BENZIL , *AMMONIUM acetate , *CANCER cells , *DRUG development - Abstract
Tetrasubstituted imidazoles were synthesized in high yields via the four-component reaction of aromatic aldehydes, amines, substituted benzils and ammonium acetate catalyzed by a porous CeO nanorod. Their anti-cancer activities on the Huh-7 hepatocellular carcinoma cell and antibacterial activities on four bacterial species (wild-type Escherichia coli, wild-type Staphylococcus aureus, Pseudomonas aeruginosa PAM1032 and Escherichia coli-NMD-1) in vitro were evaluated. One compound ( 5p) was screened out because of its high inhibition rate on all four bacterials at 100 μg/mL. Three products ( 5p, 5t and 5y) showed a high inhibition rate on the Huh-7 hepatocellular carcinoma cell at 10 μg/mL. The results indicated their potential in new drug development. [ABSTRACT FROM AUTHOR]
- Published
- 2017
- Full Text
- View/download PDF