Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors

…, A Lavecchia, M Dovizio, E Marcantoni…

文献索引：Vitale, Paola; Tacconelli, Stefania; Perrone, Maria Grazia; Malerba, Paola; Simone, Laura; Scilimati, Antonio; Lavecchia, Antonio; Dovizio, Melania; Marcantoni, Emanuela; Bruno, Annalisa; Patrignani, Paola Journal of Medicinal Chemistry, 2013 , vol. 56, # 11 p. 4277 - 4299

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被引用次数: 33

摘要

3-(5-Chlorofuran-2-yl)-5-methyl-4-phenylisoxazole (P6), a known selective cyclooxygenase- 1 (COX-1) inhibitor, was used to design a new series of 3, 4-diarylisoxazoles in order to improve its biochemical COX-1 selectivity and antiplatelet efficacy. Structure–activity relationships were studied using human whole blood assays for COX-1 and COX-2 inhibition in vitro, and results showed that the simultaneous presence of 5-methyl (or-CF3) ...