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

Article Details

Citation

Ye B, Bauman J, Chen M, Davey D, Khim SK, King B, Kirkland T, Kochanny M, Liang A, Lentz D, May K, Mendoza L, Phillips G, Selchau V, Schlyer S, Tseng JL, Wei RG, Ye H, Parkinson J, Guilford WJ

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

Bioorg Med Chem Lett. 2008 Jul 15;18(14):3891-4. doi: 10.1016/j.bmcl.2008.06.046. Epub 2008 Jun 18.

PubMed ID
18586492 [ View in PubMed
]
Abstract

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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
N-[4-(benzyloxy)phenyl]glycinamideLeukotriene A-4 hydrolaseIC 50 (nM)300N/AN/ADetails
N-[4-(benzyloxy)phenyl]glycinamideLeukotriene A-4 hydrolaseIC 50 (nM)135N/AN/ADetails