Synthesis of N-alkyl glycine amides as potent inhibitors of leukotriene A4 hydrolase期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

Synthesis of N-alkyl glycine amides as potent inhibitors of leukotriene A4 hydrolase

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

Affiliation:	^aDepartment of Medicinal Chemistry, Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, USA;^bDepartment of Molecular Pharmacology, Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, USA;^cDepartment of Immunology, Berlex Biosciences, 2600 Hilltop Drive, Richmond, CA 94804, USA

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.

Keywords:	Leukotriene A₄ Leukotriene A₄ hydrolase Anti-inflammatory Enzyme inhibitor
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