Biological evaluation and molecular docking studies of nitro benzamide derivatives with respect to in vitro anti-inflammatory activity

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• 作者：Tugba B. Tumer^a ; ^{tumerb@gmail.com} ; ^{tumertb@comu.edu.tr} ; Ferah Comert Onder^b ; Hande Ipek^a ; Tugba Gungor^b ; Seda Savranoglu^a ; Tugba Taskin Tok^c ; Ayhan Celik^d ; ¹ ; Mehmet Ay^b ; ^{mehmetay06@comu.edu.tr}
• 关键词：Nitro substituted benzamides ; Anti-inflammatory ; Nitric oxide ; iNOS ; Molecular docking
• 刊名：International Immunopharmacology
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：43
• 期：Complete
• 页码：129-139
• 全文大小：1933 K
• 卷排序：43

文摘

Six (1-6) nitro substituted benzamide derivatives were synthesized. Their anti-inflammatory activities were screened by nitric oxide inhibition assay in LPS induced RAW264.7 macrophages. Two lead compounds were identified and investigated for NO inhibitory IC50 values and dose-response relations. Molecular docking studies on iNOS enzyme supported the biological data. The effects of lead compounds on iNOS, COX-2, IL-1β and TNF-α expression were investigated.