Source:http://linkedlifedata.com/resource/pubmed/id/12749889
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
11
|
pubmed:dateCreated |
2003-5-16
|
pubmed:abstractText |
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.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Jun
|
pubmed:issn |
0960-894X
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
2
|
pubmed:volume |
13
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1879-82
|
pubmed:meshHeading |
pubmed-meshheading:12749889-Bradykinin,
pubmed-meshheading:12749889-Drug Design,
pubmed-meshheading:12749889-Isomerism,
pubmed-meshheading:12749889-Models, Molecular,
pubmed-meshheading:12749889-Molecular Conformation,
pubmed-meshheading:12749889-Pyrrolidines,
pubmed-meshheading:12749889-Receptors, Bradykinin
|
pubmed:year |
2003
|
pubmed:articleTitle |
Design and synthesis of novel pyrrolidine-containing bradykinin antagonists.
|
pubmed:affiliation |
Drug Discovery, Johnson & Johnson Pharmaceutical Research & Development, Welsh & McKean Roads, PO Box 776, Spring House, PA 19477-0776, USA. jlee@prdus.jnj.com
|
pubmed:publicationType |
Journal Article
|