Publication: Antifungal, cytotoxic activities and docking studies of 2,5-dimercapto-1,3,4-thiadiazole derivatives
Issued Date
2011-01-01
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19960816
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2-s2.0-80053945864
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Mahidol University
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SCOPUS
Bibliographic Citation
African Journal of Pharmacy and Pharmacology. Vol.5, No.4 (2011), 477-485
Suggested Citation
Weerasak Samee, Opa Vajragupta Antifungal, cytotoxic activities and docking studies of 2,5-dimercapto-1,3,4-thiadiazole derivatives. African Journal of Pharmacy and Pharmacology. Vol.5, No.4 (2011), 477-485. doi:10.5897/AJPP10.156 Retrieved from: https://repository.li.mahidol.ac.th/handle/20.500.14594/12827
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Title
Antifungal, cytotoxic activities and docking studies of 2,5-dimercapto-1,3,4-thiadiazole derivatives
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Abstract
A series of 2,5-dimercapto-1,3,4-thiadiazole derivatives (compounds 1 to 10) were prepared by nucleophilic substitution reaction between 2,5-dimercapto-1,3,4-thiadiazole and chloroheterocyclic compounds in methanol and in the presence of potassium carbonate (compounds 1 to 5 and 8) or metallic sodium (compounds 6, 7, 9 and 10) at room temperature. The cytotoxic activity was determined by green fluorescent protein (GFP)-based assay and anti-candida activity was determined by resazurin microplate assay (REMA). Compounds 1 to 4, 8 and 9 showed in vitro cytotoxic activities against Vero cells (African green monkey kidney). Compounds 4 and 10 exhibited anti-candida activities against Candida albicans (ATCC 90028) with IC 50 values of 1.94 and 19.10 μg/ml, respectively. Docking studies on the catalytic site of cytochrome P450 14α-demethylase were used to identify the chemical structures in the molecule responsible for cytotoxic and anti-candida activities of the synthesized compounds. © 2011 Academic Journals.