Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of β-amyloid1-42 secretion

…, P Misiano, C Bigogno, A Rizzi, B Riccardi…

文献索引：Peretto, Ilaria; Radaelli, Stefano; Parini, Carlo; Zandi, Michele; Raveglia, Luca F.; Dondio, Giulio; Fontanella, Laura; Misiano, Paola; Bigogno, Chiara; Rizzi, Andrea; Riccardi, Benedetta; Biscaioli, Marcello; Marchetti, Silvia; Puccini, Paola; Catinella, Silvia; Rondelli, Ivano; Cenacchi, Valentina; Bolzoni, Pier Tonino; Caruso, Paola; Villetti, Gino; Facchinetti, Fabrizio; Del Giudice, Elda; Moretto, Nadia; Imbimbo, Bruno P. Journal of Medicinal Chemistry, 2005 , vol. 48, # 18 p. 5705 - 5720

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被引用次数: 116

摘要

Flurbiprofen, a nonsteroidal antiinflammatory drug (NSAID), has been recently described to selectively inhibit β-amyloid1-42 (Aβ42) secretion, the most toxic component of the senile plaques present in the brain of Alzheimer patients. The use of this NSAID in Alzheimer's disease (AD) is hampered by a significant gastrointestinal toxicity associated with cyclooxygenase (COX) inhibition. New flurbiprofen analogues were synthesized, with the ...