Synthesis and Biological Evaluation of N‐aryl‐4‐aryl‐1,3‐Thiazole‐2‐Amine Derivatives as Direct 5‐Lipoxygenase Inhibitors

doi:10.1111/j.1747-0285.2012.01371.x

Paper

Synthesis and Biological Evaluation of N‐aryl‐4‐aryl‐1,3‐Thiazole‐2‐Amine Derivatives as Direct 5‐Lipoxygenase Inhibitors

Published Jul 1, 2012 · J. Suh, E. Yum, H. Cheon

Chemical Biology & Drug Design

Q2 SJR score

24

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0

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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.

Study Snapshot

N-aryl-4-aryl-1,3-thiazole-2-amine derivatives show potent anti-inflammatory activity by directly inhibiting 5lipoxygenase, a key enzyme involved in inflammation-related diseases like asthma and rheumatoid arthritis.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Synthesis and Biological Evaluation of N‐aryl‐4‐aryl‐1,3‐Thiazole‐2‐Amine Derivatives as Direct 5‐Lipoxygenase Inhibitors

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