Discovery of novel and potent aryl diamines as leukotriene A 4 hydrolase inhibitors

…, L Mendoza, G Phillips, JL Tseng, RG Wei, H Ye…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 14 p. 3895 - 3898

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Citation Number: 9

Abstract

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.