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

The synthesis and biological evaluation of a series of N-alkyl glycine amide analogs as LTA 4-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 pot...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 18; no. 14; pp. 3891 - 3894
Main Authors 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.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 2008
Subjects
Anti-inflammatory
Enzyme inhibitor
Leukotriene A 4
Leukotriene A 4 hydrolase
Leukotriene A 4
Leukotriene A 4 hydrolase
Enzyme inhibitor
Anti-inflammatory
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Summary:The synthesis and biological evaluation of a series of N-alkyl glycine amide analogs as LTA 4-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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2008.06.046