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Bioorg Med Chem Lett ; 19(1): 119-22, 2009 Jan 01.
Article in English | MEDLINE | ID: mdl-19014884

ABSTRACT

The synthesis and identification of sulfonamido-aryl ethers as potent bradykinin B1 receptor antagonists from a approximately 60,000 member encoded combinatorial library are reported. Two distinct series of compounds exhibiting different structure-activity relationships were identified in a bradykinin B1 whole-cell receptor-binding assay. Specific examples exhibit K(i) values of approximately 10nM.


Subject(s)
Bradykinin B1 Receptor Antagonists , Ethers/chemical synthesis , Sulfonamides/chemical synthesis , Animals , Cell Line , Combinatorial Chemistry Techniques , Humans , Small Molecule Libraries , Structure-Activity Relationship , Sulfonamides/pharmacology
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