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Synthesis and Structure−Activity Relationship of a New Series of COX-2 Selective Inhibitors: 1,5-Diarylimidazoles

Almansa, Carmen ; Alfón, José ; de Arriba, Alberto F ; Cavalcanti, Fernando L ; Escamilla, Ignasi ; Gómez, Luis A ; Miralles, Agustí ; Soliva, Robert ; Bartrolí, Javier ; Carceller, Elena ; Merlos, Manuel ; García-Rafanell, Julián

Journal of medicinal chemistry, 2003-07, Vol.46 (16), p.3463-3475 [Periódico revisado por pares]

Washington, DC: American Chemical Society

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Título:
Synthesis and Structure−Activity Relationship of a New Series of COX-2 Selective Inhibitors: 1,5-Diarylimidazoles
Autor: Almansa, Carmen ; Alfón, José ; de Arriba, Alberto F ; Cavalcanti, Fernando L ; Escamilla, Ignasi ; Gómez, Luis A ; Miralles, Agustí ; Soliva, Robert ; Bartrolí, Javier ; Carceller, Elena ; Merlos, Manuel ; García-Rafanell, Julián
Assuntos: Analgesics - chemical synthesis ; Analgesics - chemistry ; Analgesics - pharmacology ; Animals ; Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis ; Anti-Inflammatory Agents, Non-Steroidal - chemistry ; Anti-Inflammatory Agents, Non-Steroidal - pharmacology ; Arthritis, Experimental - drug therapy ; Binding Sites ; Biological and medical sciences ; Bones, joints and connective tissue. Antiinflammatory agents ; Cell Line ; Cyclooxygenase 2 ; Cyclooxygenase 2 Inhibitors ; Cyclooxygenase Inhibitors - chemical synthesis ; Cyclooxygenase Inhibitors - chemistry ; Cyclooxygenase Inhibitors - pharmacology ; Dinoprostone - biosynthesis ; Humans ; Imidazoles - chemical synthesis ; Imidazoles - chemistry ; Imidazoles - pharmacology ; Inflammation - metabolism ; Isoenzymes - antagonists & inhibitors ; Male ; Medical sciences ; Membrane Proteins ; Models, Molecular ; Pain Measurement ; Peptic Ulcer - chemically induced ; Pharmacology. Drug treatments ; Prostaglandin-Endoperoxide Synthases ; Rats ; Rats, Inbred Lew ; Rats, Sprague-Dawley ; Structure-Activity Relationship ; Sulfonamides - chemical synthesis ; Sulfonamides - chemistry ; Sulfonamides - pharmacology
É parte de: Journal of medicinal chemistry, 2003-07, Vol.46 (16), p.3463-3475
Notas: istex:03031864E0B6BEBFAD027998439E8E30C144D9F3
ark:/67375/TPS-1QKRT1CF-T
Descrição: The synthesis and the pharmacological activity of a series of 1,5-diarylimidazoles developed as potent and selective cyclooxygenase-2 (COX-2) inhibitors are described. The new compounds were evaluated both in vitro (COX-1 and COX-2 inhibition in human whole blood) and in vivo (carrageenan-induced paw edema, air-pouch, and hyperalgesia tests). Modification of all the positions of two regioisomeric imidazole cores led to the identification of 4-[4-chloro-5-(3-fluoro-4-methoxyphenyl)imidazol-1-yl]benzenesulfonamide (UR-8880, 51f) as the best candidate, which is now undergoing Phase I clinical trials.
Editor: Washington, DC: American Chemical Society
Idioma: Inglês

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Synthesis and Structure−Activity Relationship of a New Series of COX-2 Selective Inhibitors: 1,5-Diarylimidazoles

Almansa, Carmen ; Alfón, José ; de Arriba, Alberto F ; Cavalcanti, Fernando L ; Escamilla, Ignasi ; Gómez, Luis A ; Miralles, Agustí ; Soliva, Robert ; Bartrolí, Javier ; Carceller, Elena ; Merlos, Manuel ; García-Rafanell, Julián

Washington, DC: American Chemical Society

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