本文選題：-苯并硫氮雜卓　切入點(diǎn)：抑真菌活性　出處：《高等學(xué)�；瘜W(xué)學(xué)報(bào)》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(duì)稱合成方法制備了18個(gè)具有光學(xué)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(jīng)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(zhì)譜表征了其結(jié)構(gòu),通過單晶X射線衍射法確定化合物9h的相對(duì)構(gòu)型;用抑菌圈法測試了目標(biāo)化合物對(duì)新生隱球菌的抑菌活性.研究結(jié)果表明,由S型手性助劑誘導(dǎo)不對(duì)稱合成的雜卓對(duì)新生隱球菌的抑制作用普遍高于由R型手性助劑誘導(dǎo)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(xiàn)其對(duì)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(xué)化學(xué)與材料科學(xué)學(xué)院;河北師范大學(xué)生命科學(xué)學(xué)院;
【基金】：國家自然科學(xué)基金(批準(zhǔn)號(hào):20972040)資助~~
【分類號(hào)】：O621.3

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本文編號(hào)：1604387