Study on the substituents' effects of a series of synthetic chalcones against the yeast Candida albicans.
A large series of chalcones were synthesized and studied for activity against Candida albicans. The SAR analysis showed that the antifungal activity was highly dependent on the substitution pattern of the aryl rings and correlated to a large extent with the ability of compounds to interact with sulfhydryl groups. The most active were the hydroxylated chalcones as their activity related to the location of the phenolic group in the aryl ring B as follows: o-OH>p-OH approximately 3,4-di-OH>m-OH. These and other correlations obtained strongly contribute to the knowledge for design of anticandidal chalcones.
Batovska
D
D
Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Acad. G. Bonchev Street, Building 9, Sofia 1113, Bulgaria. danibat@orgchm.bas.bg <danibat@orgchm.bas.bg>
Parushev
St
S
Slavova
A
A
Bankova
V
V
Tsvetkova
I
I
Ninova
M
M
Najdenski
H
H
D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects*; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015169:Colony Count, Microbial; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D047188:Chalcones