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

J Suh, EK Yum, HG Cheon…

Index: Suh, Jeehee; Yum, Eul Kgun; Cheon, Hyae Gyeong; Cho, Young Sik Chemical Biology and Drug Design, 2012 , vol. 80, # 1 p. 89 - 98

Full Text: HTML

Citation Number: 13

Abstract

Biological evaluation of N-aryl-4-aryl-1, 3-thiazole-2-amine derivatives was examined for anti-inflammat ory activity in in vitro and in vivo assays. The thiazole compounds showed direct inhibition of 5-li poxygenase (LOX) that is a key enzyme of leukotrienes synthesis and involved in the inflammationrelated diseases, including asthma and rheumatoid arthritis. To optimize biological activity, we synthesized 1, 3-thiazole-2-amine derivatives and ...