Fungicide activity of 5-(4-chlorobenzylidene)-(Z)-2-dimethylamino-1,3-thiazol-4-one against Cryptococcus neoformans.
The present work describes the synthesis and antifungal evaluation of new 5-arylidene-(Z)-2-dimethylamino-1,3-thiazol-4-ones 4a-f, obtained by the reaction of aromatic aldehydes 1 and rhodanine 2 followed by treatment with DMF. All compounds were tested against a panel of yeasts, hialohyphomycetes, and dermatophytes using the microbroth dilution method. Compounds 4a and 4c showed antifungal activity, with compound 4a being the most active one. Compound 4a demonstrated to be fungicidal rather than fungistatic and selective activity against Cryptococcus neoformans and dermatophytes. MIC(100), MIC(80), and MIC(50) of 4a were determined against a panel of clinical isolates of C. neoformans showing ranges of MICs between 2 and 16 microg/mL.
Insuasty
Braulio
B
Department of Biology and Chemistry, Universidad Tecnológica del Chocó, Quibdó, Colombia. brainsu@univalle.edu.co
Gutiérrez
Alexander
A
Quiroga
Jairo
J
Abonia
Rodrigo
R
Nogueras
Manuel
M
Cobo
Justo
J
Svetaz
Laura
L
Raimondi
Marcela
M
Zacchino
Susana
S
D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D003883:Arthrodermataceae / Q000187:drug effects; D003455:Cryptococcus neoformans / Q000187:drug effects* / Q000302:isolation & purification; D006801:Humans; D008826:Microbial Sensitivity Tests; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology*
D000935:Antifungal Agents; D013844:Thiazoles