title: In vitro antifungal activity of sanguinarine and chelerythrine derivatives against phytopathogenic fungi.
abstract: 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
authors.affiliation: College of Science, Northwest A&F University, Yangling 712100, Shaanxi, China.
authors.forename: Xin-Juan
authors.initials: XJ
authors.lastname: Yang
authors.forename: Fang
authors.initials: F
authors.lastname: Miao
authors.forename: Yao
authors.initials: Y
authors.lastname: Yao
authors.forename: Fang-Jun
authors.initials: FJ
authors.lastname: Cao
authors.forename: Rui
authors.initials: R
authors.lastname: Yang
authors.forename: Yan-Ni
authors.initials: YN
authors.lastname: Ma
authors.forename: Bao-Fu
authors.initials: BF
authors.lastname: Qin
authors.forename: Le
authors.initials: L
authors.lastname: Zhou
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D001203:Ascomycota / Q000187:drug effects*; D053119:Benzophenanthridines / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D007546:Isoquinolines / Q000737:chemistry / Q000494:pharmacology*; D050296:Microbial Viability / Q000187:drug effects; D003904:Mitosporic Fungi / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013827:Thiabendazole / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; D053119:Benzophenanthridines; D007546:Isoquinolines; C005705:sanguinarine; C016299:chelerythrine; D013827:Thiabendazole