关键词: 1,2,4-三唑类衍生物;合成;选择性环氧化酶-2抑制剂;抗炎, 1, 2, 4-三唑类衍生物, 合成, 选择性环氧化酶-2抑制剂, 抗炎

Abstract:

Nonsteroidal anti-inflammatory durgs(NSAIDs) are among the most widely prescribed medications with their uses limited by significant toxicity.  The studies of the cyclooxygenase(COX)  show that the side effects of classical NSAIDs come from the inhibition of COX-1, while the therapeutic effects come from the inhibition of COX-2.  Selective COX-2 inhibitors were developed as NSAIDs which display the profiles of good potent activities and low side effects.  In order to search for the new NSAIDs, using the marketed selective COX-2 inhibitor celecoxib as a leading compound and based on the result of molecular modeling study of  COX-2 inhibitors, a series of novel diaryl-substituted-1,2,4-trizole derivatives were designed and synthesized.  All the target compounds were confirmed by IR, MS, ¹H NMR spectra and elemental analysis.  The results of preliminary pharmacological tests in vivo show that some compounds have certain anti-inflammatory effect.

Key words: 1,2,4-Trizole derivatives; Synthesis; Selective COX-2 inhibitors; Anti-inflammatory, 1,2,4-Trizole derivatives, Synthesis, Selective COX-2 inhibitors, Anti-inflammatory