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Synthesis of new oxadiazole derivatives as anti-inflammatory, analgesic, and antimicrobial agents

机译:合成新的恶二唑衍生物作为抗炎药,止痛药和抗菌剂

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摘要

In search of pharmalogically active molecules in the class of oxadiazoles, the present article deals with the synthesis of 5-(5'-fluoro-2'-methoxybiphenyl-3-yl)-l,3,4-oxadiazol-2(3if)-one 2 from its hydrazide analog 1. The compound 2 was regioselectively N-alkylated with alkyl halides and produced the compounds 3a-f. Compound 3f was further functionalized with substituted benzenesulfo-nyl chlorides to give compounds 3g-j. The synthesized compounds were characterized by elemental and spectral analysis. Newly synthesized compounds were tested for their in vivo anti-inflammatory, analgesic, and in vitro antimicrobial activities. The compounds 3a-c were found to have promising anti-inflammatory and analgesic activities. Compounds 3b, 3f, and 3g showed significant antibacterial and antifungal activities.
机译:为了寻找恶二唑类的药理活性分子,本文涉及5-(5'-氟-2'-甲氧基联苯-3-基)-1,3,4-恶二唑-2(3if)的合成-来自酰肼类似物1的-2。将化合物2与烷基卤化物区域选择性地N-烷基化,得到化合物3a-f。将化合物3f进一步用取代的苯磺酰氯进行官能化,得到化合物3g-j。通过元素分析和光谱分析对合成的化合物进行了表征。测试了新合成的化合物的体内抗炎,镇痛和体外抗菌活性。发现化合物3a-c具有有希望的抗炎和止痛活性。化合物3b,3f和3g显示出显着的抗菌和抗真菌活性。

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