Thalidomide analogues: Tumor necrosis factor-alpha inhibitors and their evaluation as anti-inflammatory agents

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• 作者：Juan José ; Casal^a ; ¹ ; Mariela Bollini^a ; ¹ ; Marí ; a Elisa Lombardo^b ; ^{elombardo@qb.fcen.uba.ar" class="auth_mail" title="E-mail the corresponding author} ; Ana Marí ; a Bruno^a ; ^{anabruno@ffyb.uba.ar" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Phthalimides ; Phthalazinone derivate ; TNF-α ; Anti-inflammatory effect
• 刊名：European Journal of Pharmaceutical Sciences
• 出版年：2016
• 出版时间：15 February 2016
• 年：2016
• 卷：83
• 期：Complete
• 页码：114-119
• 全文大小：492 K

文摘

A series of related thalidomide derivatives (2–9) were synthesized by microwave irradiation and evaluated for anti-inflammatory activity. Such activity was assessed in vivo and ex vivo. Compounds 2, 8 and 9 showed the highest levels of inhibition of TNF-α production. On rat paw edema and hyperalgesia assays, compound 9, (1,4-phthalazinedione) demonstrated the highest in vivo anti-inflammatory activity. Thus, compound 9 can be considered as a promising compound to be subjected to further modification to obtain new agents for the treatment of inflammatory diseases.