946576-06-3Relevant academic research and scientific papers
Berberrubine Derivatives Having Antifungal Activities
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Page/Page column 9, (2010/12/18)
The present invention relates to a berberrubine derivative having superior antifungal activity, more particularly to a berberrubine derivative having inhibitory activity against chitin synthase, which participates in the synthesis of chitin and is essenti
Synthesis and antifungal activity of a novel series of 13-(4- isopropylbenzyl)berberine derivatives
Park, Ki Duk,Cho, Sung Jin,Moon, Jae Sun,Kim, Sung Uk
supporting information; experimental part, p. 6551 - 6554 (2010/12/19)
By replacing the methyl group of 13-(4-isopropylbenzyl)berberine 2 with various acyl, alkyl, and benzyl groups via the demethylated intermediate, 13-(4-isopropylbenzyl)berberrubine 4, a novel series of 9-O-alkyl-13-(4- isopropylbenzyl)berberine derivatives was synthesized and examined for antifungal activities against various human pathogenic fungi. The introduction of various alkyl groups led to enhanced antifungal activity but that of acyl groups resulted in decrease of the activity. Among them, 9-O-butyl-13-(4- isopropylbenzyl)berberine 6d exhibited the most potent antifungal activities against Cryptococcus neoformans, Candida species (MIC = 0.25-1 μg/ml), and Aspergillus species (MIC = 2-4 μg/ml). The compound was found to be relatively safe up to 900 mg/kg in oral administration to mice.
