Synthesis of N-alkyl glycine amides as potent inhibitors of leukotriene A 4 hydrolase

…, A Liang, D Lentz, K May, L Mendoza, G Phillips…

Index: Ye, Bin; Bauman, John; Chen, Ming; Davey, David; Khim, Seock-Kyu; King, Beverly; Kirkland, Thomas; Kochanny, Monica; Liang, Amy; Lentz, Dao; May, Karen; Mendoza, Lisa; Phillips, Gary; Selchau, Victor; Schlyer, Sabine; Tseng, Jih-Lie; Wei, Robert G.; Ye, Hong; Parkinson, John; Guilford, William J. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 14 p. 3891 - 3894

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Citation Number: 13

Abstract

The synthesis and biological evaluation of a series of N-alkyl glycine amide analogs as LTA4-h inhibitors and the importance of the introduction of a benzoic acid group to the potency and pharmacokinetic parameters of our analogs are described. The lead compound in the series, 4q, has excellent potency and oral bioavailability.