J. Suh, E. Yum, H. Cheon
Jul 1, 2012
Citations
0
Influential Citations
21
Citations
Journal
Chemical Biology & Drug Design
Abstract
Biological evaluation of N‐aryl‐4‐aryl‐1,3‐thiazole‐2‐amine derivatives was examined for anti‐inflammatory activity in in vitro and in vivo assays. The thiazole compounds showed direct inhibition of 5‐lipoxygenase (LOX) that is a key enzyme of leukotrienes synthesis and involved in the inflammation‐related diseases, including asthma and rheumatoid arthritis. To optimize biological activity, we synthesized 1,3‐thiazole‐2‐amine derivatives and investigated for structure and activity relationship. Especially, N‐(3,5‐dimethylphenyl)‐4‐(4‐chlorophenyl)‐1,3‐thiazole‐2‐amine was shown to have a potent anti‐inflammatory activity as a 5‐LOX inhibitor.