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.
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.
López
S N
SN
Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, (2000), Rosario, Argentina.
Castelli
M V
MV
Zacchino
S A
SA
Domínguez
J N
JN
Lobo
G
G
Charris-Charris
J
J
Cortés
J C
JC
Ribas
J C
JC
Devia
C
C
Rodríguez
A M
AM
Enriz
R D
RD
D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002473:Cell Wall / Q000187:drug effects* / Q000378:metabolism; D002599:Chalcone / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005069:Evaluation Studies as Topic; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D011108:Polymers; D012441:Saccharomyces cerevisiae / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D011108:Polymers; D002599:Chalcone