title: Antimicrobial and cytotoxicity potential of acetamido, amino and nitrochalcones.
abstract: Chalcones constitute one of the major classes of natural products belonging to the flavonoid family, and they have been reported as having a range of important therapeutic activities, including some chalcones are effective as antimicrobial agents. Currently, the search for new structures with antimicrobial activity has been intensified due to the emergence of many strains resistant to antibiotics currently used to treat infectious diseases.3 chalcone series (amino, acetamido and nitrochalcones) were prepared (23 compounds) and evaluated for their antimicrobial and cytotoxic potential. The effects of substituents on their respective activities also was evaluated.The results showed that 4 aminochalcones (2, 4, 8, 9), 3 acetoamidochalcones (10, 14, 18) and 3 nitrochalcones (20, 22, 23), exhibited antifungal effects. The aminochalcones were more toxic than the acetamidochalcones, while the nitrochalcones did not present any toxic effect. It was verified that there seems to be structure-activity correlation in some electron-donating and withdrawing substituents groups in rings A and B of the synthetized chalcone analogues and its antifungal and cytotoxic activity.
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade do Vale do Itajaí, Itajaí, Brazil.
authors.forename: T C
authors.initials: TC
authors.lastname: Tristão
authors.forename: F
authors.initials: F
authors.lastname: Campos-Buzzi
authors.forename: R
authors.initials: R
authors.lastname: Corrêa
authors.forename: R C B
authors.initials: RC
authors.lastname: Cruz
authors.forename: V
authors.initials: V
authors.lastname: Cechinel Filho
authors.forename: A
authors.initials: A
authors.lastname: Bella Cruz
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001156:Artemia; D047188:Chalcones / Q000138:chemical synthesis* / Q000494:pharmacology*; D003470:Culture Media; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D021281:Quantitative Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D047188:Chalcones; D003470:Culture Media