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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
22
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pubmed:dateCreated |
2007-10-25
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pubmed:abstractText |
The important role of cyclooxygenase-2 (COX-2) in the pathogenesis of inflammation and side effect limitations of current COX-2 inhibitor drugs illustrates a need for the design of new compounds based on alternative structural templates. We previously reported a set of substituted 1,5-diarylpyrrole derivatives, along with their inhibitory activity toward COX enzymes. Several compounds proved to be highly selective COX-2 inhibitors and their affinity data were rationalized through docking simulations. In this paper, we describe the synthesis of new 1,5-diarylpyrrole derivatives that were assayed for their in vitro inhibitory effects toward COX isozymes. Among them, the ethyl-2-methyl-5-[4-(methylsulfonyl)phenyl]-1-[3-fluorophenyl]-1H-pyrrol-3-acetate (1d), which was the most potent and COX-2 selective compound, also showed a very interesting in vivo anti-inflammatory and analgesic activity, laying the foundations for developing new lead compounds that could be effective agents in the armamentarium for the management of inflammation and pain.
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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 |
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AnzellottiPaolaP,
pubmed-author:AnziniMaurizioM,
pubmed-author:BiavaMariangelaM,
pubmed-author:BottaMaurizioM,
pubmed-author:CappelliAndreaA,
pubmed-author:ForliStefanoS,
pubmed-author:GhelardiniCarlaC,
pubmed-author:MakovecFrancescoF,
pubmed-author:ManettiFabrizioF,
pubmed-author:PatrignaniPaolaP,
pubmed-author:PergolaCarloC,
pubmed-author:PoceGiovannaG,
pubmed-author:PorrettaGiulio CesareGC,
pubmed-author:RossiAntoniettaA,
pubmed-author:RoviniMicheleM,
pubmed-author:SautebinLidiaL,
pubmed-author:SupinoSibillaS,
pubmed-author:VivoliElisaE
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
50
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5403-11
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pubmed:meshHeading |
pubmed-meshheading:17915854-Acetates,
pubmed-meshheading:17915854-Adult,
pubmed-meshheading:17915854-Animals,
pubmed-meshheading:17915854-Carrageenan,
pubmed-meshheading:17915854-Cell Line,
pubmed-meshheading:17915854-Cyclooxygenase 1,
pubmed-meshheading:17915854-Cyclooxygenase 2,
pubmed-meshheading:17915854-Cyclooxygenase 2 Inhibitors,
pubmed-meshheading:17915854-Dinoprostone,
pubmed-meshheading:17915854-Edema,
pubmed-meshheading:17915854-Female,
pubmed-meshheading:17915854-Humans,
pubmed-meshheading:17915854-Male,
pubmed-meshheading:17915854-Mice,
pubmed-meshheading:17915854-Models, Molecular,
pubmed-meshheading:17915854-Pain Measurement,
pubmed-meshheading:17915854-Pyrroles,
pubmed-meshheading:17915854-Radioimmunoassay,
pubmed-meshheading:17915854-Rats,
pubmed-meshheading:17915854-Rats, Sprague-Dawley,
pubmed-meshheading:17915854-Rats, Wistar,
pubmed-meshheading:17915854-Structure-Activity Relationship,
pubmed-meshheading:17915854-T-Box Domain Proteins
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pubmed:year |
2007
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pubmed:articleTitle |
Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.
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pubmed:affiliation |
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università La Sapienza, piazzale Aldo Moro 5, I-00185 Roma, Italy. mariangela.biava@uniroma1.it
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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