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Synthesis, in vitro/in vivo antifungal evaluation and structure-activity relationship study of 3(2H)-pyridazinones.

作者信息

Károlyházy László, Freile Monica, Anwair Massud N, Beke Gyula, Giannini Fernando, Castelli María V, Sortino Maximiliano, Ribas Juan C, Zacchino Susana, Mátyus Péter, Enriz Ricardo D

机构信息

Departement of Organic Chemistry, Semmelweis University, Budapest, Hungary.

出版信息

Arzneimittelforschung. 2003;53(10):738-43. doi: 10.1055/s-0031-1299820.

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.

摘要

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