Design and synthesis of novel pyrrolidine-containing bradykinin antagonists

J Lee, C Reynolds, MC Jetter, MA Youngman…

文献索引：Lee, Jung; Reynolds, Charles; Jetter, Michele C.; Youngman, Mark A.; Hlasta, Dennis J.; Dax, Scott L.; Stone, Dennis J.; Zhang, Sui-Po; Codd, Ellen E. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 11 p. 1879 - 1882

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被引用次数: 11

摘要

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 B2 receptor-binding assay with a Ki of 33nM. The opposite isomer,(R)-II, had a Ki of 46nM. The in vitro binding data confirmed our ...