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pubmed-article:12749889pubmed:abstractTextThe 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.lld:pubmed
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pubmed-article:12749889pubmed:articleTitleDesign and synthesis of novel pyrrolidine-containing bradykinin antagonists.lld:pubmed
pubmed-article:12749889pubmed:affiliationDrug Discovery, Johnson & Johnson Pharmaceutical Research & Development, Welsh & McKean Roads, PO Box 776, Spring House, PA 19477-0776, USA. jlee@prdus.jnj.comlld:pubmed
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