Discovery of novel and potent aryl diamines as leukotriene A4 hydrolase inhibitors
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- 作者：Seock-Kyu Khim ; John Bauman ; Jarred Evans ; Beverly Freeman ; Beverly King ; Thomas Kirkl ; Monica Kochanny ; Dao Lentz ; Amy Liang ; Lisa Mendoza ; Gary Phillips ; Jih-Lie Tseng ; Robert G. Wei ; Hong Ye ; Lime
- 关键词：Leukotriene A4 ; LTA4 ; Leukotriene A4 hydrolase ; Enzyme inhibitor ; Antiinflammatory
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：15 July 2008
- 年：2008
- 卷：18
- 期：14
- 页码：3895-3898
- 全文大小：188 K
文摘
The synthesis and biological evaluation of a series of aryl diamines as inhibitors of LTA4-h inhibitors are described. The optimization which led to the identification of the optimal para-substitution on the diphenyl ether moiety and diamine spacer is discussed. The resulting compounds such as 3l have excellent enzyme and cellular potency as well as desirable pharmacokinetic properties.