Linked Life Data

15341491

Source:http://linkedlifedata.com/resource/pubmed/id/15341491

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
19
pubmed:dateCreated
2004-9-2
pubmed:abstractText
We describe the synthesis of new high affinity and selective A(3)-adenosine receptor (A(3)-AdoR) agonists. Introduction of a methyl group at the N(6)-position of the A(2A)-AdoR selective 2-pyrazolyl-adenosine analogues (Figure 2) brought about a substantial increase in the A(3)-AdoR binding affinity and selectivity. While the N(6)-desmethyl analogues 3a and 4 were inactive at the A(3)-AdoR (K(i) > 10 microM), the corresponding N(6)-methyl analogues 5 and 22 showed good binding affinity at the A(3)-AdoR (K(i) = 73 and 97 nM, respectively). Replacement of the carboxamide group in 5 with different heteroaryl groups resulted in analogues with high affinities and selectivity for the A(3)-AdoR. (2R,3S,4R)-tetrahydro-2-(hydroxymethyl)-5-(6-(methylamino)-2-(4-(pyridin-2-yl)-1H-pyrazol-1-yl)-9H-purin-9-yl)furan-3,4-diol (15, K(i) = 2 nM) displayed high selectivity for the A(3)-AdoR versus A(1)- and A(2A)-AdoRs (selectivity ratios of 1900 and >2000, respectively).
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
9
pubmed:volume
47
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
4766-73
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed:year
2004
pubmed:articleTitle
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.
pubmed:affiliation
Department of Bioorganic Chemistry, CV Therapeutics Inc., 3172 Porter Drive, Palo Alto, California 94304, USA. elfatih.elzein@cvt.com
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't