Design, synthesis and molecular docking studies of some 1-(5-(2-fluoro-5-(trifluoromethoxy)phenyl)-1,2,4-oxadiazol-3-yl)piperazine derivatives as potential anti-inflammatory agents

被引:8
|
作者
Kulkarni, B. [1 ]
Manjunatha, K. [1 ,2 ]
Joy, Muthipeedika Nibin [3 ]
Sajith, Ayyiliath Meleveetil [4 ]
Prashantha, C. N. [5 ]
Pakkath, Ranjith [4 ]
Alshammari, Mohammed B. [6 ]
机构
[1] Bharathiar Univ, Res & Dev Ctr, Coimbatore 641046, Tamil Nadu, India
[2] Nagarjuna Coll Engn & Technol, Dept Chem, Bengaluru 562164, Karnataka, India
[3] Ural Fed Univ, Innovat Ctr Chem & Pharmaceut Technol, Inst Chem Technol, 19 Mira St, Ekaterinburg 620002, Russia
[4] Kannur Univ, Sch Chem Sci, Payyanur Campus,PO 670327, Kannur, Kerala, India
[5] Reva Univ, Sch Appl Sci, Dept Biotechnol, Bengaluru 560064, Karnataka, India
[6] Prince Sattam Bin Abdulaziz Univ, Coll Sci & Humanities, Chem Dept, POB 83, Al Kharij 11942, Saudi Arabia
关键词
Oxadiazole; Anti-inflammatory activity; Molecular docking; SAR; BIOLOGICAL EVALUATION; INHIBITORS; AMIDE;
D O I
10.1007/s11030-021-10340-1
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
We herein report the facile synthesis of a series of 3,5-substituted-1,2,4-oxadiazole derivatives in good to excellent yields. The anti-inflammatory potential of the newly synthesized compounds was evaluated by anti-denaturation assay using diclofenac sodium as the reference standard. Some of the compounds exhibited profound activity profile when compared to the standard drug. The molecular docking and SAR studies were carried out at the later stage for gaining more insights about the promising activity profile of the synthesized molecules.
引用
收藏
页码:2893 / 2905
页数:13
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