|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
20
|
|
pubmed:dateCreated |
2004-9-21
|
|
pubmed:abstractText |
The synthesis and SAR of a new class of piperidine-based alphavbeta3/alphavbeta5 integrin antagonists is described. Replacement of an amide bond in a prototype isonipecotamide by a C-C isostere, and adjustment of the spacer length between the carboxylic acid and basic moieties, led to low nanomolar antagonists of alphavbeta3 and/or alphavbeta5 integrins with excellent selectivity versus alpha(IIb)beta3.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Oct
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:BakerJudithJ,
pubmed-author:BrunnerLiviaL,
pubmed-author:BurnsCandaceC,
pubmed-author:DamianoBruce PBP,
pubmed-author:De CorteBart LBL,
pubmed-author:GalemmoRobert ARAJr,
pubmed-author:GhoshShyamaliS,
pubmed-author:HoekstraWilliam JWJ,
pubmed-author:JohnsonDana LDL,
pubmed-author:JosKK,
pubmed-author:KinneyWilliam AWA,
pubmed-author:MaryanoffBruce EBE,
pubmed-author:ProostJef CJC,
pubmed-author:SantulliRosemary JRJ,
pubmed-author:ToungeBrett ABA,
pubmed-author:TumanRobert WRW
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
18
|
|
pubmed:volume |
14
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
5227-32
|
|
pubmed:dateRevised |
2006-11-15
|
|
pubmed:meshHeading |
pubmed-meshheading:15380233-Administration, Oral,
pubmed-meshheading:15380233-Animals,
pubmed-meshheading:15380233-Biological Availability,
pubmed-meshheading:15380233-Humans,
pubmed-meshheading:15380233-Integrin alphaVbeta3,
pubmed-meshheading:15380233-Integrins,
pubmed-meshheading:15380233-Piperidines,
pubmed-meshheading:15380233-Propionic Acids,
pubmed-meshheading:15380233-Protein Binding,
pubmed-meshheading:15380233-Rats,
pubmed-meshheading:15380233-Receptors, Vitronectin,
pubmed-meshheading:15380233-Structure-Activity Relationship
|
|
pubmed:year |
2004
|
|
pubmed:articleTitle |
Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins.
|
|
pubmed:affiliation |
Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, Welsh & McKean Roads, Spring House, PA 19477-0776, USA. bdecorte@prdus.jnj.com
|
|
pubmed:publicationType |
Journal Article,
Comparative Study
|
