The study of novel peptide-based endothelin receptor antagonists

摘要

From the SAR studies, we concluded that the linear peptide-based ET receptor antagonists synthesized in our laboratory with following features might show high activities: (1) R group showed crucial function in improving its selectivity and affinity to ET receptor. ABO showed high ET_A receptor binding activity than others. DAD showed high hydrophilicity, that it could improve the solubility of these antagonists; (2) the first amino acid AA_1 showed high hydrophobic dependence, it was the same as the report in literature; (3) the second amino acid AA_2 can be aromatic hydrophobic amino acid. D-Trp and its derivative showed high activity in the antagonists; (4) the third amino acid AA_3 should be D-isomer, L-amino acid did not show inhibitory activity in this study.