Twenty chalcone derivatives were designed and synthesized with a view to developing novel anticandidal agents. All the compounds were evaluated for their antifungal activity against Candida albicans (ATCC 10231 and ten clinical isolates). Most of them exhibited moderate anticandidal potency with MIC values ranging from 2.0 to 32.0 μg/mL. Four compounds (T4, T6, T19, T20) displayed potent anticandidal activity with MIC values of 2.0 μg/mL. Compound T6 showed the most potent activity against Candida albicans (ATCC 10231 and four clinical isolates). In addition, attempts have also been made to correlate anticandidal activity to physicochemical properties. The results indicated that incorporation of halogen on the benzene ring is beneficial for anticandidal activity.
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Acknowledgment
This project was supported by the National Natural Science Foundation (NNSF) of China (Grant No. 81302641) and the Natural Science Basic Research Plan in Shaanxi Province of China (Program No. 2011K15-05-02).
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Published in Khimiya Prirodnykh Soedinenii, No. 4, July–August, 2015, pp. 536–540.
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Shan, Y., Lei, J., Zhang, L. et al. Design, Synthesis, and Biological Evaluation of Chalcone Derivatives as Novel Anticandidal Agents. Chem Nat Compd 51, 620–625 (2015). https://doi.org/10.1007/s10600-015-1369-6
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DOI: https://doi.org/10.1007/s10600-015-1369-6