|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
23
|
|
pubmed:dateCreated |
2008-11-13
|
|
pubmed:abstractText |
The design synthesis and SAR of a series of chiral ring-constrained norepinephrine reuptake inhibitors with improved physicochemical properties is described. Typical compounds are potent (IC(50)s<10 nM), selective against the other monoamine transporters, weak CYP2D6 inhibitors (IC(50)s>1 microM) and stable to oxidation by human liver microsomes. In addition, the compounds exhibit a favorable polarity profile.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Dec
|
|
pubmed:issn |
1464-3405
|
|
pubmed:author |
pubmed-author:AparicioAnnaA,
pubmed-author:ChingBrettB,
pubmed-author:EwingToddT,
pubmed-author:FleckBeth ABA,
pubmed-author:GaoYinghongY,
pubmed-author:GenicotMarc JMJ,
pubmed-author:GogasKathleenK,
pubmed-author:HudsonSarahS,
pubmed-author:PontilloJosephJ,
pubmed-author:WadeWarren SWS,
pubmed-author:WangHuaH,
pubmed-author:WenJennyJ,
pubmed-author:WuDongpeiD
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
1
|
|
pubmed:volume |
18
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
6151-5
|
|
pubmed:meshHeading |
pubmed-meshheading:18954981-Combinatorial Chemistry Techniques,
pubmed-meshheading:18954981-Cytochrome P-450 CYP2D6,
pubmed-meshheading:18954981-Drug Design,
pubmed-meshheading:18954981-Humans,
pubmed-meshheading:18954981-Indans,
pubmed-meshheading:18954981-Inhibitory Concentration 50,
pubmed-meshheading:18954981-Microsomes, Liver,
pubmed-meshheading:18954981-Molecular Structure,
pubmed-meshheading:18954981-Neurotransmitter Uptake Inhibitors,
pubmed-meshheading:18954981-Norepinephrine,
pubmed-meshheading:18954981-Propylamines,
pubmed-meshheading:18954981-Stereoisomerism,
pubmed-meshheading:18954981-Structure-Activity Relationship
|
|
pubmed:year |
2008
|
|
pubmed:articleTitle |
Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics.
|
|
pubmed:affiliation |
Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
|
|
pubmed:publicationType |
Journal Article
|
