title: Synthesis, bioevaluation and structural study of substituted phthalazin-1(2H)-ones acting as antifungal agents.
abstract: Twenty-five polysubstituted phthalazinone derivatives were synthesized and tested for their antifungal activity against a panel of pathogenic and clinically important yeasts and filamentous fungi. Among them, the compound 4-(4-chlorobenzyl)-2-methylphthalazin-1(2H)-one (5) exhibited a remarkable antifungal activity against standardised strains of dermatophytes and Cryptococcus neoformans, as well as against some clinical isolates. A physicochemical study performed on compound 5 revealed its conformational and electronic characteristics, providing us with useful data for the future design of novel related antifungal analogues.
authors.affiliation: Pharmacognosy Department, Faculty of Biochemical and Pharmaceutical Sciences, National University of Rosario, Suipacha 531, 2000 Rosario, Argentine. mgderita@hotmail.com
authors.forename: Marcos
authors.initials: M
authors.lastname: Derita
authors.forename: Esther
authors.initials: E
authors.lastname: Del Olmo
authors.forename: Bianca
authors.initials: B
authors.lastname: Barboza
authors.forename: Ana Esther
authors.initials: AE
authors.lastname: García-Cadenas
authors.forename: José Luis
authors.initials: JL
authors.lastname: López-Pérez
authors.forename: Sebastián
authors.initials: S
authors.lastname: Andújar
authors.forename: Daniel
authors.initials: D
authors.lastname: Enriz
authors.forename: Susana
authors.initials: S
authors.lastname: Zacchino
authors.forename: Arturo
authors.initials: A
authors.lastname: San Feliciano
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D003883:Arthrodermataceae / Q000187:drug effects; D003198:Computer Simulation; D003455:Cryptococcus neoformans / Q000187:drug effects; D006801:Humans; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D008968:Molecular Conformation; D010084:Oxidation-Reduction; D010793:Phthalazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011789:Quantum Theory; D013499:Surface Properties; D013816:Thermodynamics
chemical_list: D000935:Antifungal Agents; D010793:Phthalazines