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rdf:type |
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lifeskim:mentions |
umls-concept:C0001962,
umls-concept:C0002771,
umls-concept:C0003209,
umls-concept:C0014994,
umls-concept:C0205314,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0243072,
umls-concept:C0679083,
umls-concept:C0679622,
umls-concept:C1515655,
umls-concept:C1515999,
umls-concept:C1521991,
umls-concept:C1522290,
umls-concept:C1533691,
umls-concept:C1883254
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pubmed:issue |
17
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pubmed:dateCreated |
2008-9-4
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pubmed:abstractText |
Following our previous research on anti-inflammatory drugs (NSAIDs), we report here the synthesis of chiral 1,5-diarylpyrroles derivatives that were characterized for their in vitro inhibitory effects toward cyclooxygenase (COX) isozymes. Analysis of enzymatic affinity and COX-2 selectivity led us to the selection of one compound (+/-)-10b that was further tested in vitro in the human whole blood (HWB) and in vivo for its anti-inflammatory activity in mice. The affinity data have been rationalized through docking simulations.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Acetic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Alcohols,
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics,
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Inflammatory Agents...,
http://linkedlifedata.com/resource/pubmed/chemical/Carrageenan,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclooxygenase 1,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclooxygenase 2,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Ethers,
http://linkedlifedata.com/resource/pubmed/chemical/Isoenzymes,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrroles
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
1464-3391
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pubmed:author |
pubmed-author:AnzellottiPaolaP,
pubmed-author:AnziniMaurizioM,
pubmed-author:BiavaMariangelaM,
pubmed-author:BottaMaurizioM,
pubmed-author:CirilliRobertoR,
pubmed-author:FerrettiRosellaR,
pubmed-author:ForliStefanoS,
pubmed-author:GallinellaBrunoB,
pubmed-author:GhelardiniCarlaC,
pubmed-author:GiordaniAntonioA,
pubmed-author:La TorreFrancescoF,
pubmed-author:MakovecFrancescoF,
pubmed-author:ManettiFabrizioF,
pubmed-author:NorciniMonicaM,
pubmed-author:PatrignaniPaolaP,
pubmed-author:PergolaCarloC,
pubmed-author:PoceGiovannaG,
pubmed-author:PorrettaGiulio CGC,
pubmed-author:RossiAntoniettaA,
pubmed-author:SautebinLidiaL,
pubmed-author:SupinoSibillaS
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
8072-81
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pubmed:meshHeading |
pubmed-meshheading:18752957-Acetic Acid,
pubmed-meshheading:18752957-Alcohols,
pubmed-meshheading:18752957-Analgesics,
pubmed-meshheading:18752957-Animals,
pubmed-meshheading:18752957-Anti-Inflammatory Agents, Non-Steroidal,
pubmed-meshheading:18752957-Binding Sites,
pubmed-meshheading:18752957-Carrageenan,
pubmed-meshheading:18752957-Cells, Cultured,
pubmed-meshheading:18752957-Computer Simulation,
pubmed-meshheading:18752957-Cyclooxygenase 1,
pubmed-meshheading:18752957-Cyclooxygenase 2,
pubmed-meshheading:18752957-Dose-Response Relationship, Drug,
pubmed-meshheading:18752957-Drug Evaluation, Preclinical,
pubmed-meshheading:18752957-Edema,
pubmed-meshheading:18752957-Enzyme Activation,
pubmed-meshheading:18752957-Enzyme Inhibitors,
pubmed-meshheading:18752957-Ethers,
pubmed-meshheading:18752957-Humans,
pubmed-meshheading:18752957-Isoenzymes,
pubmed-meshheading:18752957-Male,
pubmed-meshheading:18752957-Mice,
pubmed-meshheading:18752957-Models, Chemical,
pubmed-meshheading:18752957-Molecular Structure,
pubmed-meshheading:18752957-Pain,
pubmed-meshheading:18752957-Pain Measurement,
pubmed-meshheading:18752957-Pyrroles,
pubmed-meshheading:18752957-Rats,
pubmed-meshheading:18752957-Rats, Sprague-Dawley,
pubmed-meshheading:18752957-Rats, Wistar,
pubmed-meshheading:18752957-Stereoisomerism,
pubmed-meshheading:18752957-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.
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pubmed:affiliation |
Dipartimento di Studi di Chimica e Tecnologie del Farmaco, Università La Sapienza, Piazzale Aldo Moro, 5, I-00185 Roma, Italy.
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pubmed:publicationType |
Journal Article
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