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Merck
CN
  • Design and synthesis of some thiazolyl and thiadiazolyl derivatives of antipyrine as potential non-acidic anti-inflammatory, analgesic and antimicrobial agents.

Design and synthesis of some thiazolyl and thiadiazolyl derivatives of antipyrine as potential non-acidic anti-inflammatory, analgesic and antimicrobial agents.

Bioorganic & medicinal chemistry (2008-12-17)
Sherif A F Rostom, Ibrahim M el-Ashmawy, Heba A Abd el Razik, Mona H Badr, Hayam M A Ashour
摘要

The synthesis of two groups of structure hybrids comprising basically the antipyrine moiety attached to either polysubstituted thiazole or 2,5-disubstituted-1,3,4-thiadiazole counterparts through various linkages is described. Twelve out of the newly synthesized compounds were evaluated for their anti-inflammatory activity using two different screening protocols; namely, the formalin-induced paw edema and the turpentine oil-induced granuloma pouch bioassays, using diclofenac Na as a reference standard. The ulcerogenic effects and acute toxicity (ALD(50)) values of these compounds were also determined. Meanwhile, the analgesic activity of the same compounds was evaluated using the rat tail withdrawal technique. Additionally, the synthesized compounds were evaluated for their in vitro antimicrobial activity. In general, compounds belonging to the thiazolylantipyrine series exhibited better biological activities than their thiadiazolyl structure variants. Collectively, compounds 6, 10, 26, and 27 proved to display distinctive anti-inflammatory and analgesic profiles with a fast onset of action. All of the tested compounds revealed super GI safety profile and are well tolerated by the experimental animals with high safety margin (ALD(50)>3.0 g/kg). Meanwhile, compounds 7, 10, 11, and 23 are considered to be the most active broad spectrum antimicrobial members in this study. Compound 10 could be identified as the most biologically active member within this study with an interesting dual anti-inflammatory analgesic and antibacterial profile.

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Sigma-Aldrich
双氯芬酸 钠盐
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货号包装规格是否有货价格数量
25 g
国内现货,预计发货时间 April 18, 2025
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CN¥416.55
100 g
国内现货,预计发货时间 April 18, 2025
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CN¥696.70
Sigma-Aldrich
氨苄西林 三水合物, 900-1050 μg/mg anhydrous basis (HPLC)
登录查看公司和协议定价
货号包装规格是否有货价格数量
25 g
国内现货,预计发货时间 April 18, 2025
详情...
CN¥416.55
100 g
国内现货,预计发货时间 April 18, 2025
详情...
CN¥696.70