N-Benzoyl amino acids as LFA-1/ICAM inhibitors 1: Amino acid structure–activity relationship

…, M Beresini, K Clark, RS McDowell, JC Marsters…

文献索引：Burdick, Daniel J.; Paris, Ken; Weese, Kenneth; Stanley, Mark; Beresini, Maureen; Clark, Kevin; McDowell, Robert S.; Marsters Jr., James C.; Gadek, Thomas R. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 6 p. 1015 - 1018

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被引用次数: 20

摘要

The association of ICAM-1 with LFA-1 plays a critical role in several autoimmune diseases. N-2-Bromobenzoyl l-tryptophan, compound 1, was identified as an inhibitor to the formation of the LFA-1/ICAM complex. The SAR of the amino acid indicates that the carboxylic acid is required for inhibition and that l-histidine is the most favored amino acid.