Linked Life Data

18243711

Source:http://linkedlifedata.com/resource/pubmed/id/18243711

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
7
pubmed:dateCreated
2008-4-14
pubmed:abstractText
After the CB1 receptor antagonist SR141716 (rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. Several series of urea, carbamate, amide, sulfonamide and oxalamide derivatives based on 1-benzhydrylpiperazine scaffold were synthesized and tested for CB1 receptor binding affinity. The SAR studies to optimize the CB1 binding affinity led to the potent urea derivatives. After the additional SAR studies to optimize the substituents of diphenyl rings, the combination of 2-chlorophenyl and 4-chlorophenyl turned out to be the most potent scaffold. The CB2 binding affinity assay as well as functional assay was also conducted on these compounds. Herein we wish to introduce several novel CB1 antagonists with IC(50) values less than 100 nM for the CB1 receptor binding.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
1464-3391
pubmed:author
pubmed:issnType
Electronic
pubmed:day
1
pubmed:volume
16
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
4035-51
pubmed:meshHeading
pubmed:year
2008
pubmed:articleTitle
Design, synthesis and biological evaluation of piperazine analogues as CB1 cannabinoid receptor ligands.
pubmed:affiliation
Small Molecule Group, Central Research Institute, Green Cross Corporation, 341 Bojeong-dong, Giheung-gu, Yongin, Gyunggi-do 446-799, Republic of Korea.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't