|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0053139,
umls-concept:C0184511,
umls-concept:C0205360,
umls-concept:C0243192,
umls-concept:C0311400,
umls-concept:C0439097,
umls-concept:C0441655,
umls-concept:C0700307,
umls-concept:C1533691,
umls-concept:C1547348,
umls-concept:C1705241,
umls-concept:C1880355
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|
pubmed:issue |
21
|
|
pubmed:dateCreated |
2009-10-12
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|
pubmed:abstractText |
We have investigated phenol replacements in a series of diaryl amino piperidine delta opioid agonists. From this study we have demonstrated that the hydroxy functional group can be replaced with a primary amide group, giving enhanced activity at the delta receptor, increased selectivity versus mu and kappa as well as improved in vitro metabolic stability.
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|
pubmed:language |
eng
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|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
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pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Nov
|
|
pubmed:issn |
1464-3405
|
|
pubmed:author |
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
1
|
|
pubmed:volume |
19
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
5999-6003
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|
pubmed:meshHeading |
pubmed-meshheading:19800790-Analgesics,
pubmed-meshheading:19800790-Animals,
pubmed-meshheading:19800790-Diphenylamine,
pubmed-meshheading:19800790-Humans,
pubmed-meshheading:19800790-Microsomes, Liver,
pubmed-meshheading:19800790-Piperidines,
pubmed-meshheading:19800790-Rats,
pubmed-meshheading:19800790-Receptors, Opioid, delta,
pubmed-meshheading:19800790-Structure-Activity Relationship
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|
pubmed:year |
2009
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|
pubmed:articleTitle |
Delta agonist hydroxy bioisosteres: the discovery of 3-((1-benzylpiperidin-4-yl){4-[(diethylamino)carbonyl]phenyl}amino)benzamide with improved delta agonist activity and in vitro metabolic stability.
|
|
pubmed:affiliation |
Department of Medicinal Chemistry, AstraZeneca R&D Montréal, 7171 Frédérick-Banting, Ville St. Laurent, Québec, Canada H4S 1Z9. andrew.griffin@astrazeneca.com
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pubmed:publicationType |
Journal Article
|
