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Synthesis and Antimicrobial Activity of Calycanthaceous Derivatives
Natural Product Communications ( IF 1.5 ) Pub Date : 2021-09-13 , DOI: 10.1177/1934578x211032611
Rui Zhu 1, 2 , Cheng Yang 2 , Ke Han 2 , Yongdong Gu 2 , Jiwen Zhang 3 , Shaojun Zheng 2 , Hongjin Bai 1
Affiliation  

A series of calycanthaceous alkaloid analogs have been synthesized in excellent yields. All the target compounds were evaluated in vitro for biological activity against a broad range of plant pathogen fungi, bacteria and human pathogenic fungi, and some of the designed compounds exhibited potential activity in the primary assays. Notably, Compound b7 illustrated higher degrees of activity against Aspergillu sflavu than amphotericin B, with a minimal inhibitory concentration value of 15.63 µg·mL−1. Compound b7 displayed the most effective activity among the tested calycanthaceous analogs and might be a novel potential leading compound for further development of antifungal agent.



中文翻译:

花萼衍生物的合成及抗菌活性

已经以极好的收率合成了一系列花萼生物碱类似物。所有目标化合物都在体外评估了对多种植物病原体真菌、细菌和人类病原体真菌的生物活性,并且一些设计的化合物在初步分析中表现出潜在的活性。值得注意的是,化合物b7显示出比两性霉素B更高的针对黄曲霉的活性,最小抑制浓度值为15.63μg ·mL -1。化合物b7在测试的花萼类似物中表现出最有效的活性,可能是进一步开发抗真菌剂的新型潜在先导化合物。

更新日期:2021-09-13
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