Author/Authors :
Seock-Kyu Khim، نويسنده , , John Bauman، نويسنده , , Jarred Evans، نويسنده , , Beverly Freeman، نويسنده , , Beverly King، نويسنده , , Thomas Kirkland، نويسنده , , Monica Kochanny، نويسنده , , Dao Lentz، نويسنده , , Amy Liang، نويسنده , , Lisa Mendoza، نويسنده , , Gary Phillips، نويسنده , , Jih-Lie Tseng، نويسنده , , Robert G. Wei، نويسنده , , Hong Ye، نويسنده , , Limei Yu، نويسنده , , John Parkinson، نويسنده , , William J. Guilford، نويسنده ,
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.
Keywords :
Antiinflammatory , Leukotriene A4 , LTA4 , Enzyme inhibitor , leukotriene A4 hydrolase