title: Synthesis, in vitro/in vivo antifungal evaluation and structure-activity relationship study of 3(2H)-pyridazinones.
abstract: The synthesis, in vitro/in vivo antifungal evaluation and a structure-activity relationship (SAR) study of 3(2H)-pyridazinones was carried out. The results reported here may be helpful in the structural identification and understanding of the minimum structural requirements for these molecules acting as antifungal agents. In addition, the most active structure in this series was tested for its capacity of inhibiting Saccharomyces cerevisiae beta 1,3-glucan synthase and chitin synthase, enzymes that catalyze the synthesis of the major polymers of the fungal cell wall.
authors.affiliation: Departement of Organic Chemistry, Semmelweis University, Budapest, Hungary.
authors.forename: László
authors.initials: L
authors.lastname: Károlyházy
authors.forename: Monica
authors.initials: M
authors.lastname: Freile
authors.forename: Massud N
authors.initials: MN
authors.lastname: Anwair
authors.forename: Gyula
authors.initials: G
authors.lastname: Beke
authors.forename: Fernando
authors.initials: F
authors.lastname: Giannini
authors.forename: María V
authors.initials: MV
authors.lastname: Castelli
authors.forename: Maximiliano
authors.initials: M
authors.lastname: Sortino
authors.forename: Juan C
authors.initials: JC
authors.lastname: Ribas
authors.forename: Susana
authors.initials: S
authors.lastname: Zacchino
authors.forename: Péter
authors.initials: P
authors.lastname: Mátyus
authors.forename: Ricardo D
authors.initials: RD
authors.lastname: Enriz
mesh_terms: D000287:Administration, Topical; D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D003883:Arthrodermataceae / Q000187:drug effects; D002687:Chitin Synthase / Q000037:antagonists & inhibitors; D003881:Dermatomycoses / Q000188:drug therapy / Q000382:microbiology; D005658:Fungi / Q000187:drug effects*; D006168:Guinea Pigs; D007202:Indicators and Reagents; D007654:Ketoconazole / Q000494:pharmacology; D008297:Male; D008826:Microbial Sensitivity Tests; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D012441:Saccharomyces cerevisiae / Q000187:drug effects / Q000201:enzymology; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D007202:Indicators and Reagents; D011724:Pyridazines; D002687:Chitin Synthase; D007654:Ketoconazole