rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
10
|
pubmed:dateCreated |
2003-5-5
|
pubmed:abstractText |
Three series of spirocyclopiperazinium derivatives 5a-d, 6a-f and 17a-d were synthesized and evaluated for their in vivo analgesic activities. Compounds 5a, 17a and 17b exhibited excellent analgesic activity. Two important structure-activity relationships were observed from this study: (1) the quaternary ammonium functionality is a critical pharmacophore for analgesic activity; (2) it is important to adjust the lipophilic property of compounds to improve analgesic activity.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
May
|
pubmed:issn |
0960-894X
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
19
|
pubmed:volume |
13
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1729-32
|
pubmed:dateRevised |
2010-11-18
|
pubmed:meshHeading |
pubmed-meshheading:12729652-Analgesics,
pubmed-meshheading:12729652-Animals,
pubmed-meshheading:12729652-Dose-Response Relationship, Drug,
pubmed-meshheading:12729652-Hydrophobic and Hydrophilic Interactions,
pubmed-meshheading:12729652-Hypnotics and Sedatives,
pubmed-meshheading:12729652-Maximum Tolerated Dose,
pubmed-meshheading:12729652-Mice,
pubmed-meshheading:12729652-Piperazines,
pubmed-meshheading:12729652-Salts,
pubmed-meshheading:12729652-Spiro Compounds,
pubmed-meshheading:12729652-Structure-Activity Relationship
|
pubmed:year |
2003
|
pubmed:articleTitle |
Unique spirocyclopiperazinium salt. Part 2: synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics.
|
pubmed:affiliation |
School of Pharmaceutical Sciences, Peking University, Beijing 100083, PR China.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|