Synthesis and biological evaluation of N-aryl-4-aryl-1,3-thiazole-2-amine derivatives as direct 5-lipoxygenase inhibitors.

Article Details

Citation

Suh J, Yum EK, Cheon HG, Cho YS

Synthesis and biological evaluation of N-aryl-4-aryl-1,3-thiazole-2-amine derivatives as direct 5-lipoxygenase inhibitors.

Chem Biol Drug Des. 2012 Jul;80(1):89-98. doi: 10.1111/j.1747-0285.2012.01371.x. Epub 2012 Apr 13.

PubMed ID
22404847 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ZileutonArachidonate 5-lipoxygenaseIC 50 (nM)1807.425Details