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Synthesis and Biological Evaluation of a New Series of Pyrazolines as New Anticandidal Agents

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Pharmaceutical Chemistry Journal Aims and scope

New pyrazoline derivatives bearing an oxadiazole moiety were synthesized via the reaction of 1-(chloroacetyl)-3-(2-furyl/thienyl)-5-aryl-2-pyrazolines with 5-substituted-1,3,4-oxadiazole-2(3H)-thiones in the presence of potassium carbonate. Compounds 1 – 32 were screened for their antifungal activity against various Candida species and compared with ketoconazole. Among these compounds, the most effective derivatives were evaluated for their cytotoxicity against NIH/3T3 cells. 2-({2-[5-(4-Bromophenyl)-3-(2-furyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl}thio)-5-(2-cyclopentylethyl)-1,3,4-oxadiazole (23) can be identified as the most potent antifungal agent against C. tropicalis due to its inhibitory effect on C. tropicalis and low toxicity to NIH/3T3 cells.

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Acknowledgements

This study was supported by Anadolu University Scientific Research Projects Commission under the grant no. 1001S41.

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Authors and Affiliations

  1. Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 26470, Eskişehir, Turkey

    Ahmet Özdemir, Mehlika Dilek Altıntop, Zafer Asım Kaplancıklı & Gülhan Turan-Zitouni

  2. Anadolu University, Graduate School of Health Sciences, 26470, Eskişehir, Turkey

    Zafer Asım Kaplancıklı

  3. Anadolu University, Faculty of Pharmacy, Department of Biochemistry, 26470, Eskişehir, Turkey

    Gülşen Akalın Çiftçi

  4. Anadolu University, Faculty of Pharmacy, Department of Pharmacognosy, 26470, Eskişehir, Turkey

    Fatih Demirci

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  1. Ahmet Özdemir
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  2. Mehlika Dilek Altıntop
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Correspondence to Ahmet Özdemir.

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Özdemir, A., Altıntop, M.D., Kaplancıklı, Z.A. et al. Synthesis and Biological Evaluation of a New Series of Pyrazolines as New Anticandidal Agents. Pharm Chem J 48, 603–612 (2014). https://doi.org/10.1007/s11094-014-1158-8

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  • DOI: https://doi.org/10.1007/s11094-014-1158-8

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