Life SciencesMedicinal ChemistryMicrobiologyDrug DiscoveryMycologyStructure-activity RelationshipsAntifungal AgentsFungal Secondary MetabolitesMedicinal PlantsStructure-activity Relationship AnalysisBotanical BioassaysChemical Structure-activity RelationshipsEffective Concentration MedianFungal Bioactive CompoundsMedian Effective DoseMycelial GrowthNatural Antifungal CompoundsNew Antifungal Agents
In order to understand the antifungal activity of some derivatives of sanguinarine (S) and chelerythrine (C) and their structure-activity relationships, sixteen derivatives of S and C were prepared and evaluated for in vitro antifungal activity against seven phytopathogenic fungi by the mycelial growth rate method. The results showed that S, C and their 6-alkoxy dihydro derivatives S₁-S₄, C₁-C₄ and 6-cyanodihydro derivatives S₅, C₅ showed significant antifungal activity at 100 µg/mL against all the tested fungi. For most tested fungi, the median effective concentrations of S, S₁, C and C₁ were in a range of 14-50 µg/mL. The structure-activity relationship showed that the C=N+ moiety was the determinant for the antifungal activity of S and C. S₁-S₅ and C₁-C₅ could be considered as the precursors of S and C, respectively. Thus, the present results strongly suggested that S and C or their derivatives S₁-S₅ and C₁-C₅ should be considered as good lead compounds or model molecules to develop new anti-phytopathogenic fungal agents. can't login to work station for 2hrs--took 2 hrs vacation
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The Benzophenanthridine Alkaloids
Barry D. Krane, Moses O. Fagbule, Maurice Shamma et al. · Journal of Natural Products · 1984 · 279 citations
Biologically active natural products
K. L. Rinehart, Ryuichi Sakai, Tom G. Holt et al. · Pure and Applied Chemistry · 1990 · 183 citations · Full text
Pharmacy, Medicinal Chemistry, Natural Product Biosynthesis +6