Please use this identifier to cite or link to this item: https://ir.swu.ac.th/jspui/handle/123456789/14589
ชื่อเรื่อง: Antifungal, cytotoxic activities and docking studies of 2,5-dimercapto-1,3,4-thiadiazole derivatives
ผู้แต่ง: Samee W.
Vajragupta O.
Keywords: alanine
amphotericin B
ellipticine
heterocyclic compound
histidine
isoleucine
leucine
methanol
methionine
potassium carbonate
resazurin
sterol 14alpha demethylase
sterol 14alpha demethylase inhibitor
thiadiazole derivative
tyrosine
unclassified drug
valine
voriconazole
animal cell
antifungal activity
article
binding site
Candida albicans
catalysis
chemical structure
controlled study
crystal structure
drug activity
drug cytotoxicity
drug structure
drug synthesis
enzyme active site
hydrophobicity
IC 50
in vitro study
infrared spectroscopy
mass spectrometry
molecular docking
nonhuman
nucleophilicity
room temperature
วันที่เผยแพร่: 2011
บทคัดย่อ: 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 IC50 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.
URI: https://ir.swu.ac.th/jspui/handle/123456789/14589
https://www.scopus.com/inward/record.uri?eid=2-s2.0-80053945864&doi=10.5897%2fAJPP10.156&partnerID=40&md5=93c8b9f852d11a6f1eab854bd8f3f512
ISSN: 19960816
Appears in Collections:Scopus 1983-2021

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