合成;“3-(2-[1H苯并咪唑-2-酰基)-2-氧乙基]苯基)乙酸及其衍生物的表征及抗炎活性”

R. Bhor, Sonali Pawar
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引用次数: 0

摘要

通过苯- 1,2二胺与甲酸反应,合成一系列苯并咪唑类五元杂环,形成各种苯并咪唑衍生物(BD- BK)化合物,并采用大鼠足水肿法测定其抗炎活性。所有合成的化合物都通过1HNMR, IR和一些质谱数据进行了表征。用重结晶法对化合物进行了纯化。整个化合物具有良好的抗炎活性:苯并咪唑(AA), 1-(1h -苯并咪唑-2-基)-2-(3-羟基苯基)乙酮(AC);2-{3-[2-(1h -苯并咪唑-2-基)-2-氧乙基]苯基}- n -苯乙酰胺;2-{3-[2-(1h -苯并咪唑-2-基)-2-氧乙基]苯基}- n -(2-硝基苯基)乙酰胺(AK);2-{3-[2-(1h -苯并咪唑-2-基)-2-氧乙基]苯基}- n -(3-硝基苯基)乙酰胺(AL)。吲哚美辛被用作标准药物,并与新合成的药物进行了比较。一些新的合成药物已显示出较好的抗炎活性。通过与标准药物吲哚美辛的比较,确定化合物AA、AC、AJ、AK和AL的药效最强。
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Synthesis; Characterization and Anti Inflammatory Activity of “3-(2-[1H Benzimidazole-2-YL)-2-Oxethyl] Phenyl) Acetic Acid and Its Derivatives”
A series of five-membered heterocyclic rings like Benzimidazole were synthesized by the reaction between benzene-1, 2 diamine and formic acid to form various Benzimidazole derivatives (BD- BK) compounds and was tested for their anti-inflammatory activity determined by rat-paw- oedema method. All the synthesis compounds have been characterized by 1HNMR, IR and some Mass spectral data. The compounds were purified by recrystallization method. The entire compound gives good response for the anti-inflammatory activity: Benzimidazole (AA), 1-(1H-benzimidazol-2-yl)-2-(3-hydroxyphenyl) ethanone (AC); 2-{3-[2-(1H-benzimidazol-2-yl)-2-oxoethyl] phenyl}-N-phenylacetamide (AJ); 2-{3-[2-(1H-benzimidazol-2-yl)-2-oxoethyl] phenyl}-N-(2-nitrophenyl) acetamide (AK); 2-{3-[2-(1H-benzimidazol-2-yl)-2-oxoethyl] phenyl}-N-(3-nitrophenyl) acetamide (AL). For this anti-inflammatory activity, Indometacin was used as a standard drug and compared to new synthesized drugs. Some new synthesized drugs have shown better activities for the anti-inflammation. The synthesize compounds were establish to be AA to AL. The compound AA, AC, AJ, AK and AL were established to be the most potent compound through compare to standard drugs Indomethacin.
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