- Structure-activity relationship (SAR) of the α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists.
Structure-activity relationship (SAR) of the α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists.
Bioorganic & medicinal chemistry letters (2010-11-27)
Min Zhong, Emily J Hanan, Wang Shen, Minna Bui, Michelle R Arkin, Kenneth J Barr, Marc J Evanchik, Ute Hoch, Jennifer Hyde, Jose R Martell, Johan D Oslob, Kumar Paulvannan, Saileta Prabhu, Jeffrey A Silverman, Jasmin Wright, Chul H Yu, Jiang Zhu, W Mike Flanagan
PMID21109434
RESUMEN
This letter describes the structure-activity relationship (SAR) of the 'right-wing' α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists. Novel (S)-substituted heteroaryl-bearing α-amino acids have been identified as replacements of the 'right-wing' (S)-2,3-diaminopropanoic acid (DAP) moiety. Improvement of potency in the Hut-78 assay in the presence of 10% human serum has also been achieved.
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