| Literature DB >> 12749889 |
Jung Lee1, Charles Reynolds, Michele C Jetter, Mark A Youngman, Dennis J Hlasta, Scott L Dax, Dennis J Stone, Sui-Po Zhang, Ellen E Codd.
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.Entities:
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Year: 2003 PMID： 12749889 DOI： 10.1016/s0960-894x(03)00309-3
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823