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Synthesis and Biological Evaluation of Furo[3,2-c]pyrazole-5-carbimidates

机译:呋喃的合成与生物学评价[3,2-C]吡唑-5-碳纤维素

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In the present work, novel pyrazole fused dihydrofurans synthesized via a chronological addition of N-chloro succinimide and base piperidine to pyrano[3,2-c]pyrazole carbonitrile derivatives in methanol medium. Oxidative difunctionalization was done with the reagent iV-chloro succinimide by the addition of both chlorine and alkoxy groups crosswise the chromene double bond. The addition of base results in the construction of dihydrofuran derivatives by ring contraction. The structures of newly synthesized compounds were characterized on the basis of physical and spectral data. Synthesized compounds were evaluated for antibacterial and anti-inflammatory activities. All the compounds exhibited significant antibacterial activity against all the four strains of bacteria and then MICs ranged between 1.56 and 12.55 ug/mL. In anti-inflammatory screening, among all the tested compounds, compounds 7,8,9,11,12,13,14,16,17 and 18 exhibited significant protection against the edema formation at a concentration of 100 mg/kg.
机译:在本作本作中,通过按时间顺序加入N-氯琥珀酰亚胺和基哌啶在吡喃[3,2-C]吡唑碳腈衍生物中合成的新型吡唑稠合的二氢呋喃呋喃呋喃呋喃。通过加入两种氯和烷氧基横向与铬烯双键相加,用试剂IV-氯琥珀酰亚胺进行氧化双官能化。添加基础导致戒指收缩构建二氢呋喃衍生物。基于物理和光谱数据表征新合成化合物的结构。评估合成化合物以进行抗菌和抗炎活动。所有化合物对所有四种菌株表现出显着的抗菌活性,然后在1.56和12.55 ug / ml之间进行MIC。在抗炎筛选中,在所有测试的化合物中,化合物7,8,9,11,12,13,14,16,17和18在100mg / kg的浓度下表现出对水肿形成的显着保护。

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