Author/Authors :
Jung Lee، نويسنده , , Charles Reynolds، نويسنده , , Michele C. Jetter، نويسنده , , Mark A. Youngman، نويسنده , , Dennis J. Hlasta، نويسنده , , Scott L. Dax، نويسنده , , Dennis J. Stone، نويسنده , , Sui-Po Zhang، نويسنده , , Ellen E. Codd، نويسنده ,
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 B2 receptor-binding assay with a Ki of 33 nM. The opposite isomer, (R)-II, had a Ki of 46 nM. The in vitro binding data confirmed our conformational hypothesis.
