Synthesis and Biological Evaluation of N-aryl-4-aryl-1,3-Thiazole-2-Amine Derivatives as Direct 5-Lipoxygenase Inhibitors
- Authors
- Suh, Jeehee; Yum, Eul Kgun; Cheon, Hyae Gyeong; Cho, Young Sik
- Issue Date
- Jul-2012
- Publisher
- WILEY-BLACKWELL
- Keywords
- 5-lipoxygenase; anti-inflammation; leukotriene B4; neutrophil; thiazole scaffold
- Citation
- CHEMICAL BIOLOGY & DRUG DESIGN, v.80, no.1, pp.90 - 99
- Journal Title
- CHEMICAL BIOLOGY & DRUG DESIGN
- Volume
- 80
- Number
- 1
- Start Page
- 90
- End Page
- 99
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/16300
- DOI
- 10.1111/j.1747-0285.2012.01371.x
- ISSN
- 1747-0277
- 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.
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