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ID: ALA1146611
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of novel pyrrolidine-containing bradykinin antagonists.
Authors: Lee J, Reynolds C, Jetter MC, Youngman MA, Hlasta DJ, Dax SL, Stone DJ, Zhang SP, Codd EE.
Abstract: The design and synthesis of novel pyrrolidine-containing bradykinin antagonists, II, are described. Conformational analysis suggested that a pyrrolidine moiety could substitute for the N-methyl cis-amide moiety of FR 173657. The in vitro binding data showed that the (S)-isomer of II was potent in the bradykinin B(2) receptor-binding assay with a K(i) of 33 nM. The opposite isomer, (R)-II, had a K(i) of 46 nM. The in vitro binding data confirmed our conformational hypothesis.
CiteXplore: 12749889