Discovery of novel and potent aryl diamines as leukotriene A4 hydrolase inhibitors.

作者信息

Khim Seock-Kyu, Bauman John, Evans Jarred, Freeman Beverly, King Beverly, Kirkland Thomas, Kochanny Monica, Lentz Dao, Liang Amy, Mendoza Lisa, Phillips Gary, Tseng Jih-Lie, Wei Robert G, Ye Hong, Yu Limei, Parkinson John, Guilford William J

机构信息

Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, USA.

出版信息

Bioorg Med Chem Lett. 2008 Jul 15;18(14):3895-8. doi: 10.1016/j.bmcl.2008.06.041. Epub 2008 Jun 18.

DOI:10.1016/j.bmcl.2008.06.041

PMID:18590959

Abstract

The synthesis and biological evaluation of a series of aryl diamines as inhibitors of LTA(4)-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.

摘要

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