- One-pot Van Leusen synthesis of 4,5-disubstituted oxazoles in ionic liquids
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An efficient and mild protocol for the preparation of 4,5-disubstituted oxazoles through an improved one-pot van Leusen oxazole synthesis in ionic liquids is described. The oxazole products were prepared from tosylmethyl isocyanide (TosMIC), aliphatic hal
- Wu, Bo,Wen, Jun,Zhang, Ji,Li, Jing,Xiang, Yong-Zhe,Yu, Xiao-Qi
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experimental part
p. 500 - 504
(2009/08/07)
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- Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-Diarylimidazoles
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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-fluoro4-methoxyphenyl)imidazol-1-yl]benzenesulfonamide (UR-8880, 51f) as the best candidate, which is now undergoing Phase I clinical trials.
- 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
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p. 3463 - 3475
(2007/10/03)
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