本文選題：-苯并硫氮雜卓　切入點：抑真菌活性　出處：《高等學�；瘜W學報》2017年03期 　論文類型：期刊論文

【摘要】：以(R)/(S)-4-芐基-2-VA唑烷酮為手性助劑,采用不對稱合成方法制備了18個具有光學活性的2-甲氧羰基-4-氟苯基-1,5-苯并硫氮雜卓類化合物9a~9i和14a~14i,經HPLC分析e.e.值較為理想;通過核磁共振譜、紅外光譜和高分辨質譜表征了其結構,通過單晶X射線衍射法確定化合物9h的相對構型;用抑菌圈法測試了目標化合物對新生隱球菌的抑菌活性.研究結果表明,由S型手性助劑誘導不對稱合成的雜卓對新生隱球菌的抑制作用普遍高于由R型手性助劑誘導合成的雜卓及外消旋體.測試了抑菌活性較好的化合物14a~14f的最小抑菌濃度(MIC)和最小殺菌濃度(MFC),發(fā)現其對新生隱球菌的MIC和MFC均低于抗真菌藥物氟康唑.
[Abstract]:In (R) / (S) -4- benzyl -2-VA as oxazolidinone chiral auxiliary, preparation of 18 optically active 2- fluorenylmethoxycarbonyl -4- difluorophenyl -1,5- benzothiazepine compounds 9a~9i and 14a~14i by using the method of asymmetric synthesis, HPLC analysis of E.E. value ideal; by nuclear magnetic resonance spectroscopy, infrared spectroscopy high resolution mass spectrometry and characterization of its structure, determine the relative configuration of the compound 9h by single crystal X ray diffraction method; the antibacterial activity of the target compounds of Cryptococcus neoformans test by the bacteriostatic circle method. The results show that the inhibition of S induced by chiral auxiliaries in asymmetric synthesis of miscellaneous Zhuo on Cryptococcus neoformans is generally higher than that by R type of chiral auxiliaries and racemic complex Zhuo induced synthesis. The minimal inhibitory concentration of compound 14a~14f has better antibacterial activity test (MIC) and minimum bactericidal concentration (MFC), on the discovery of Cryptococcus neoformans MIC and MFC were lower than that of anti really Fluconazole, a bacterial drug.

【作者單位】： 河北師范大學化學與材料科學學院;河北師范大學生命科學學院;
【基金】：國家自然科學基金(批準號:20972040)資助~~
【分類號】：O621.3

【相似文獻】

相關期刊論文 前10條

1 王文貴;李良泉;;糖在不對稱合成中的應用[J];化學試劑;1987年02期

2 張U，

本文編號：1604387