Synthesis and biological evaluation of pyrazole chalcones and derived bipyrazoles as anti-inflammatory and antioxidant agents

被引:14
|
作者
Faidallah, Hassan M. [1 ]
Rostom, Sherif A. F. [2 ,3 ]
Khan, Khalid A. [1 ]
机构
[1] King Abdulaziz Univ, Fac Sci, Dept Chem, Jeddah 21589, Saudi Arabia
[2] King Abdulaziz Univ, Fac Pharm, Dept Pharmaceut Chem, Jeddah 21589, Saudi Arabia
[3] Univ Alexandria, Fac Pharm, Dept Pharmaceut Chem, Alexandria 21521, Egypt
关键词
Chalcones; Bipyrazoles; Sulfonylureas; Sulfonylthioureas; Anti-inflammatory; Antioxidant; ACTIVE CYCLOOXYGENASE-2 INHIBITORS; ANTIMICROBIAL AGENTS; THIOUREA DERIVATIVES; ANALGESIC AGENTS;
D O I
10.1007/s12272-014-0392-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of bipyrazoles functionalized with sulfonamide, N-1,N-3-disubstituted sulfonylurea, sulfonylthiourea pharmacophores, and some derived thiazolidinone and thiazoline ring systems were synthesized. The structures of the newly synthesized compounds were substantiated by analytical and diverse spectroscopic data. The anti-inflammatory and antioxidant activity of some of the newly synthesized compounds were tested and the results reveled that compounds 14, 16, 20, 24 and 25 proved to be the most active anti-inflammatory agents according to the Carrageenan-induced rat paw edema bioassay. Whereas, the analogs 14, 16 and 24 were able to exhibit good to moderate antioxidant activity in the DPPH radical-scavenging assay. Hence, compounds 14, 16 and 24 can be considered as lead structures for dual anti-inflammatory and antioxidant activities.
引用
收藏
页码:203 / 215
页数:13
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