|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
3
|
|
pubmed:dateCreated |
2005-12-26
|
|
pubmed:abstractText |
A series of conformationally constrained bicyclic derivatives derived from SR141716 was prepared and evaluated as hCB(1)-R antagonists and inverse agonists. Optimization of the structure-activity relationships around the 2,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one derivative 2a led to the identification of two compounds with oral activity in rodent feeding models (2h and 4a). Replacement of the PP group in 2h with other bicyclic groups resulted in a loss of binding affinity.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics,
http://linkedlifedata.com/resource/pubmed/chemical/Bicyclo Compounds, Heterocyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrazolones,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidinones,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Cannabinoid, CB1,
http://linkedlifedata.com/resource/pubmed/chemical/pyrazolone,
http://linkedlifedata.com/resource/pubmed/chemical/rimonabant
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Feb
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:BlackShawn CSC,
pubmed-author:ButlerMaryM,
pubmed-author:CarpinoPhilip APA,
pubmed-author:DayRobertR,
pubmed-author:DebartoloDemetria BDB,
pubmed-author:DibrinoJosephJ,
pubmed-author:DowRobert LRL,
pubmed-author:DutcherDarrinD,
pubmed-author:FichtnerMichael WMW,
pubmed-author:GautreauDeniseD,
pubmed-author:GriffithDavid ADA,
pubmed-author:HadcockJohn RJR,
pubmed-author:IredalePhilip APA,
pubmed-author:Kelly-SullivanDawnD,
pubmed-author:LizanoJeff SJS,
pubmed-author:O'connorRebecca ERE,
pubmed-author:RoseColin RCR,
pubmed-author:SakyaSubasS,
pubmed-author:SandsMichelle AMA,
pubmed-author:ScottDennis ODO,
pubmed-author:WardKaren MKM
|
|
pubmed:issnType |
Print
|
|
pubmed:volume |
16
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
731-6
|
|
pubmed:dateRevised |
2007-10-17
|
|
pubmed:meshHeading |
pubmed-meshheading:16263283-Analgesics,
pubmed-meshheading:16263283-Animals,
pubmed-meshheading:16263283-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:16263283-Binding Sites,
pubmed-meshheading:16263283-Feeding Behavior,
pubmed-meshheading:16263283-Models, Biological,
pubmed-meshheading:16263283-Piperidines,
pubmed-meshheading:16263283-Pyrazoles,
pubmed-meshheading:16263283-Pyrazolones,
pubmed-meshheading:16263283-Pyrimidinones,
pubmed-meshheading:16263283-Receptor, Cannabinoid, CB1,
pubmed-meshheading:16263283-Rodentia,
pubmed-meshheading:16263283-Structure-Activity Relationship
|
|
pubmed:year |
2006
|
|
pubmed:articleTitle |
New bicyclic cannabinoid receptor-1 (CB1-R) antagonists.
|
|
pubmed:affiliation |
Pfizer Global Research and Development-Groton Laboratories, Groton, CT 06340, USA. philip.a.carpino@pfizer.com
|
|
pubmed:publicationType |
Journal Article
|
