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• W3111966422 abstract "Abstract This study reports the chemo‐ and regioselective synthesis, at good yields, of ( E )‐4‐(amino)‐1,1,1‐trifluoro‐5‐(4,5‐alkyl‐3‐(trifluoromethyl)‐1 H ‐pyrazol‐1‐yl)pent‐3‐en‐2‐ones (pyrazole‐enaminones), from the of N ‐alkylation reaction of trifluoromethyl pyrazoles with 5‐bromo enaminones. The obtained compounds were tested as potential analgesics in a screening test involving mice. Three of these compounds significantly reduced the spontaneous nociception induced by the application of capsaicin, which is an algogenic substance. Compound 5 g presented satisfactory antinociceptive activity compared to celecoxib, a drug used as a positive control, without promoting locomotor changes in the mice. Moreover, molecular modeling simulations showed that compound 5 g interacts with the cyclooxygenase enzyme at the same binding site as celecoxib. Together, our data suggest that compound 5 g is a promising prototype for the development of new analgesic drugs." @default.
• W3111966422 created "2020-12-21" @default.
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• W3111966422 date "2020-12-08" @default.
• W3111966422 modified "2023-10-16" @default.
• W3111966422 title "Pyrazole‐Enaminones as Promising Prototypes for the Development of Analgesic Drugs" @default.
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• W3111966422 doi "https://doi.org/10.1002/slct.202004049" @default.
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