Synthesis, in vitro/in vivo Antifungal Evaluation and Structure-Activity Relationship Study of 3(2H) Pyridazinones

L.KÁROLYHÁZY; M.L FREILE; M.ANWAIR; G.BEKE; F.GIANNINI; M.CASTELLI; M.SORTINO; J.RIBAS; S.ZACCHINO; P.MATYUS; ENRIZ R D

ARZNEIMITTEL FORSCHUNG DRUG RESEARCH

ECV-EDITIO CANTOR VERLAG MEDIZIN NATURWISSENSCHAFTEN

Año: 2003 vol. 53 p. 738 - 743

0004-4172

The synthesis, in vitro/in vivo antifungal evaluation anda 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 ofthe mínimum structural requirements for these molecules acting as antifungalagents. In addition, the most active structure in this series was tested for its capa-city of inhibiting Saccharomyces cerevisiae Pl,3-glucan synthase and chitin synthase, enzymes that catalyze the synthesis of the major polymers of thefungal cell wall.