In vitro antifungal evaluation and structure-activity relationships of a new series of chalcone derivatives and synthetic analogues, with inhibitory properties against polymers of the fungal cell wall

S N López; M V Castelli; S A Zacchino; J N Domínguez; G Lobo; J Charris-Charris; J C Cortés; J C Ribas; C Devia; A M Rodríguez; R D Enriz

doi:10.1016/s0968-0896(01)00116-x

In vitro antifungal evaluation and structure-activity relationships of a new series of chalcone derivatives and synthetic analogues, with inhibitory properties against polymers of the fungal cell wall

Bioorg Med Chem. 2001 Aug;9(8):1999-2013. doi: 10.1016/s0968-0896(01)00116-x.

Authors

S N López¹, M V Castelli, S A Zacchino, J N Domínguez, G Lobo, J Charris-Charris, J C Cortés, J C Ribas, C Devia, A M Rodríguez, R D Enriz

Affiliation

¹ Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, (2000), Rosario, Argentina.

PMID: 11504637
DOI: 10.1016/s0968-0896(01)00116-x

Abstract

Here we report the synthesis, in vitro antifungal evaluation and SAR study of 41 chalcones and analogues. In addition, all active structures were tested for their 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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antifungal Agents / chemical synthesis
Antifungal Agents / chemistry
Antifungal Agents / pharmacology*
Cell Wall / drug effects*
Cell Wall / metabolism
Chalcone / chemical synthesis
Chalcone / chemistry
Chalcone / pharmacology*
Evaluation Studies as Topic
Microbial Sensitivity Tests
Molecular Conformation
Polymers
Saccharomyces cerevisiae / drug effects*
Saccharomyces cerevisiae / metabolism
Structure-Activity Relationship

Substances

Antifungal Agents
Polymers
Chalcone