کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1356002 1500460 2014 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
1,3,4-Trisubstituted pyrazole analogues as promising anti-inflammatory agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
1,3,4-Trisubstituted pyrazole analogues as promising anti-inflammatory agents
چکیده انگلیسی


• Four series of 1,3,4-trisubstituted pyrazole derivatives were synthesized.
• All synthesized compounds were evaluated for their anti-inflammatory activity.
• The title compound 5a showed promising anti-inflammatory activity.
• Selected compounds were investigated for their COX-2 inhibitory activity.
• Compound 5a showed potential selective COX-2 inhibitory activity.

Twenty-two 1,3,4-trisubstituted pyrazole (3a–d), (4a–d), (5a–d), (6a–l) derivatives were synthesized and structure of newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, and mass spectral analysis. These compounds were screened for the anti-inflammatory activity by carrageenan-induced paw edema method. Compounds 5a, and 5b showed excellent anti-inflammatory activity (⩾84.2% inhibition) and 3a, 3b, and 3c showed good anti-inflammatory activity (⩾64.6% inhibition) compared to that of the standard drug diclofenac (86.72%) when measured 3 h after the carrageenan injection. Moreover, the cyclooxygenase (COX) enzyme inhibitor activity of selected compounds, which are the excellent anti-inflammatory activities in carrageenan-induced paw edema model, was investigated in vitro COX inhibition assay. Molecular docking study further helped in supporting the observed activity. In addition compound 5a exhibited considerable cytotoxic activity against MCF-7 cell line with IC50 value 6.5 μM.

A series of substituted pyrazole derivatives were prepared and evaluated for their anti-inflammatory activities. Compounds 5a was identified as selective COX-2 inhibitor (COX-1 IC50 = 73 μM, COX-2 IC50 = 14 μM).Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic Chemistry - Volume 54, June 2014, Pages 51–59
نویسندگان
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