Abstract
Over the last decade, there has been a dramatic increase in the prevalence and gravity of systemic fungal diseases. This study aimed therefore at evaluating the antifungal potential of ester derivatives of benzoic and cinnamic acids from three Candida species. The compounds were prepared via Fischer esterification, and the antifungal assay was performed by the microdilution method in 96-well microplates for determining the minimal inhibitory concentrations (MICs). The findings of the antifungal tests revealed that the analogue compound methyl ferulate, methyl o-coumarate, and methyl biphenyl-3-carboxylate displayed an interesting antifungal activity against all Candida strains tested, with MIC values of 31.25-62.5, 62.5-125, and 62.5 μg/ml, respectively. A preliminary Structure-Activity Relationship study of benzoic and cinnamic acid derivatives has led to the recognition of some important structural requirements for antifungal activity. The results of molecular docking indicate that the presence of the enoate moiety along with hydroxyl and one methoxy substitution in the phenyl ring has a positive effect on the bioactivity of compound 7 against Candida albicans. These observations further support the hypothesis that the antifungal activity of compound 7 could be due to its binding to multiple targets, specifically to QR, TS, and ST-PK. Additional experiments are required in the future to test this hypothesis and to propose novel compounds with improved antifungal activity.
Highlights
In the last decade, the number and severity of systemic fungal infections has increased intensely, and this has been linked to an increased number of immunocompromised hosts, such as patients undergoing organ transplantation, receiving anticancer chemotherapy, suffering from AIDS, or in therapy with broad-spectrum antimicrobials [1, 2]
The antifungal assay was performed by the microdilution method in 96-well microplates for determining the minimal inhibitory concentrations (MICs)
In contrast to the results reported Sánchez-Maldonado and coworkers (2011) [48] observed that the antibacterial activity of hydroxybenzoic acids was enhanced through the replacement of a hydroxyl group by a methoxy group
Summary
The number and severity of systemic fungal infections has increased intensely, and this has been linked to an increased number of immunocompromised hosts, such as patients undergoing organ transplantation, receiving anticancer chemotherapy, suffering from AIDS, or in therapy with broad-spectrum antimicrobials [1, 2]. This factor, together with the limitations of available antifungal therapies and the crescent emergence of drug resistance, has created an urgent need for the development of new efficient broad-spectrum and safer antifungal agents, mainly with novel mechanisms for action [3, 4]. The most important pathogenic species of the Candida genus are C. albicans, C. parapsilosis, C. krusei, C. tropicalis, and C. glabrata [8].
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