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Citation: Tang Yanling, Liu Bei, Yang Xiaobi, Fu Liqiong, Gao Hui, Mao Zewei. Syntheses and In Vitro Anti-Inflammatory Activities of 3-Aryl-5-thienyl dihydropyrazole Sulfonamide Derivatives[J]. Chemistry, ;2019, 82(10): 942-945. shu

Syntheses and In Vitro Anti-Inflammatory Activities of 3-Aryl-5-thienyl dihydropyrazole Sulfonamide Derivatives

College of Pharmaceutical Science, Yunnan University of Chinese Medicine, Kunming 650500

Corresponding author: Mao Zewei, maozw@ynutcm.edu.cn
Received Date: 16 June 2019
Accepted Date: 26 June 2019

Figures(1)

Dihydropyrazole is an important five-membered N-heterocyclic compound with a broad range of biological activities, which widely exist in various active natural products. In this study, eight new 3-aryl-5-(2-thienyl)-4, 5-dihydro-1H-pyrazole derivatives (4a~4h) have been prepared, and their structures were characterized by IR, ¹H NMR and ¹³C NMR. The in vitro anti-inflammatory activities of title compounds have been tested by lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages. The biological results indicated that the sulfonamide derivatives 4a, 4e and 4h display potential anti-inflammatory activity. Especially compound 4a had the most inhibitory effect on NO generation (IC₅₀=12.64μmol/L, which is comparable to the positive control drug dexamethasone), and could be used as a lead compound for further studies.
- Dihydropyrazole,
- Sulfonamide derivatives,
- Anti-inflammatory activity
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