Synthesis of some novel oxadiazole and oxadiazoline analogues for their antiinflammatory activity

被引:21
|
作者
Rajak, Harish [1 ]
Kharya, Murli Dhar
Mishra, Pradeep
机构
[1] Guru Ghasidas Univ, SLT Inst Pharmaceut Sci, Bilaspur 495009, CG, India
[2] Dr Hari Singh Gour Vishwavidyalaya, Dept Pharmaceut Sci, Sagar 470003, MP, India
关键词
oxadiazole; oxadiazoline; antiinflammatory activity;
D O I
10.1248/yakushi.127.1757
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The search for newer non-steroidal antiinflammatory drugs (NSAIDs) and the importance of oxadiazoles as antiinflammatory agents prompted us to undertake the synthesis of some novel oxadiazole and related analogues with unreported antiinflammatory activities. The antiinflammatory potential of the compounds was investigated using the carrageenan-induced rat paw edema method and cotton pellet-induced granuloma method. Some compounds demonstrated marked antiinflammatory activities. The antiinflammatory activity of oxadiazoles at doses of 100 mg/kg was shown by their ability to provide 28-55%, 21-36%, and 27-491/6 protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. On the other hand, the antiinflammatory properties of oxadiazolines at doses of 100 mg/kg was reflected by their ability to provide 15-47 %, 22-39 %, and 23-47 % protection against carrageenan-induced rat paw edema, moist cotton pellet-induced, and dry cotton pellet-induced granuloma, respectively. Structure-activity relationships among synthesized compounds were also studied.
引用
收藏
页码:1757 / 1764
页数:8
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