Synthesis, in vitro/in vivo antifungal evaluation and structure-activity relationship study of 3(2H)-pyridazinones.
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.
Károlyházy
László
L
Departement of Organic Chemistry, Semmelweis University, Budapest, Hungary.
Freile
Monica
M
Anwair
Massud N
MN
Beke
Gyula
G
Giannini
Fernando
F
Castelli
María V
MV
Sortino
Maximiliano
M
Ribas
Juan C
JC
Zacchino
Susana
S
Mátyus
Péter
P
Enriz
Ricardo D
RD
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
D000935:Antifungal Agents; D007202:Indicators and Reagents; D011724:Pyridazines; D002687:Chitin Synthase; D007654:Ketoconazole