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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, characterization and in vitro antibacterial activity of new steroidal 5-en-3-oxazolo and thiazoloquinoxaline.
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Synthesis, characterization and in vitro antibacterial activity of new steroidal 5-en-3-oxazolo and thiazoloquinoxaline.

机译：新型甾体5-en-3-恶唑和噻唑并喹喔啉的合成，表征和体外抗菌活性。

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摘要

Steriodal heterocyclic systems namely cholest-5-en-3-oxazolo and thiazoloquinoxaline have been synthesized via the reaction of cholest-5-en-3-one semicarbazone/thiosemicarbazone with 2,3-dichloroquinoxaline at 80 degrees C in high yield. Cholest-5-en-3-one semicarbazone is obtained by the condensation of cholest-5-en-3-one with semicarbazide in the presence of AcONa in ethanol and cholest-5-en-one thiosemicarbazone is obtained by the condensation of cholest-5-en-3-one with thiosemicarbazide in ethanol in the presence of a few drops of HCl. The structures of these compounds were evident by elemental analysis, IR, 1H NMR and FAB mass spectral analysis. These synthesized compounds were investigated for antibacterial activity first by the disk-diffusion assay against two Gram-positive and two Gram-negative bacteria and then the minimum inhibitory concentration (MIC) of these compounds were determined and the results were compared with the standard drug Amoxicillin. The results showed that these compounds oxazolo/thiazoloquinoxaline are better antibacterial agents as compared to the standard drug Amoxicillin.
机译：胆甾型5-烯-3-酮半缩氨基脲/硫代半碳杂zone与2,3-二氯喹喔啉在80℃下以高收率反应合成了胆甾型杂环化合物，即胆甾-5-烯-3-恶唑啉和噻唑并喹喔啉。在乙醇中存在AcONa的情况下，胆甾5-3-3-1与氨基脲的缩合反应得到胆甾5-烯3-氨基脲;胆甾2-胆甾的缩合反应得到胆甾5-5-烯1硫代半脲。在数滴HCl的存在下，在乙醇中与-5- -5- -3-硫代氨基脲反应。这些化合物的结构通过元素分析，IR，1 H NMR和FAB质谱分析可见。首先通过圆盘扩散法对这些合成的化合物对两种革兰氏阳性和两种革兰氏阴性细菌的抗菌活性进行研究，然后确定这些化合物的最低抑菌浓度（MIC），并将结果与​​标准药物阿莫西林进行比较。 。结果表明，与标准药物阿莫西林相比，这些化合物恶唑啉/噻唑并喹喔啉是更好的抗菌剂。

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