Synthesis and anti-inflammatory activity evaluation of novel 3-alkyl-6-(4 H -1,2,4-triazol-4-yl)-3,4-dihydro-2 H -benzo[ e ][1,3]oxazine derivatives

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摘要：

To discover new compounds with anti-inflammatory activity, a series of novel 3-alkyl-6-(4H-1,2,4-triazol-4-yl)-3,4-dihydro-2H-benzo[e][1,3]oxazine derivatives were synthesized and their structures were confirmed by spectroscopic techniques. In vivo anti-inflammatory activity of the synthesized compounds was determined using the xylene-induced mouse ear edema model. 3-Heptyl-6-(4H-1,2,4-triazol-4-yl)-3,4-dihydro-2H-benzo[e] [1,3]oxazine and 3-p-tolyl-6-(4H-1,2,4-triazol-4-yl)-3,4-dihydro-2H-benzo[e][1,3]oxazine demonstrated higher anti-inflammatory activity (74.04% and 64.99%, respectively) at 0.5h after intraperitoneal administration than the reference drug ibuprofen (62.65%). Further, the time of peak effect after oral administration was 4h for both compounds. Our results identify new compounds with anti-inflammatory activity in vivo that may have improved safety/side effect profiles relative to the currently approved nonsteroidal anti-inflammatory drugs.

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关键词：

Synthesis Anti-inflammatory Mannich reaction 4-Aminophenol

DOI：

10.1007/s00044-016-1679-7

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年份：

2016