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Synthesis and Antifungal Activity of Chromones and Benzoxepines from the Leaves of Ptaeroxylon obliquum.
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-08-13 , DOI: 10.1021/acs.jnatprod.0c00587
Modibo S Malefo 1 , Thanyani E Ramadwa 2 , Ibukun M Famuyide 2 , Lyndy J McGaw 2 , Jacobus N Eloff 2 , Molahlehi S Sonopo 3 , Mamoalosi A Selepe 1
Affiliation  

This study reports the first total synthesis of the bioactive oxepinochromones 12-O-acetyleranthin (8) (angular isomer) and 12-O-acetylptaeroxylinol (9) (linear isomer). The antifungal activity of these compounds and their derivatives was determined against Candida albicans and Cryptococcus neoformans. Most compounds had good selectivity between the two fungi and showed moderate to good activity. 12-O-Acetyleranthin (8) had the highest activity against C. albicans, with an MIC value of 9.9 μM, while 12-O-acetylptaeroxylinol (9), the compound present in Ptaeroxylon obliquum, had the highest activity against C. neoformans, with an MIC value of 4.9 μM.

中文翻译:

椴木叶中色酮和苯并氧杂的合成及抗真菌活性。

该研究报告了具有生物活性的 oxepinochromones 12- O-乙酰基白质素 ( 8 )(角异构体)和 12- O-乙酰基ptaeroxylinol ( 9 )(线性异构体)的首次全合成。测定了这些化合物及其衍生物对白色念珠菌新型隐球菌的抗真菌活性。大多数化合物在两种真菌之间具有良好的选择性,并显示出中等至良好的活性。12- O-乙酰基花青素 ( 8 ) 对白色念珠菌的活性最高,MIC 值为 9.9 μM,而 12- O-乙酰基丁二烯酚 ( 9 ),其存在于Ptaeroxylonobliquum新型隐球菌的活性最高,MIC 值为 4.9 μM。
更新日期:2020-08-28
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