Weerasak SameeOpa VajraguptaSrinakharinwirot UniversityMahidol University2018-05-032018-05-032011-01-01African Journal of Pharmacy and Pharmacology. Vol.5, No.4 (2011), 477-485199608162-s2.0-80053945864https://repository.li.mahidol.ac.th/handle/20.500.14594/12827A 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.Mahidol UniversityPharmacology, Toxicology and PharmaceuticsArticleSCOPUS10.5897/AJPP10.156