dc.contributor.author |
Samee W. |
|
dc.contributor.author |
Vajragupta O. |
|
dc.date.accessioned |
2021-04-05T03:35:48Z |
|
dc.date.available |
2021-04-05T03:35:48Z |
|
dc.date.issued |
2011 |
|
dc.identifier.issn |
19960816 |
|
dc.identifier.other |
2-s2.0-80053945864 |
|
dc.identifier.uri |
https://ir.swu.ac.th/jspui/handle/123456789/14589 |
|
dc.identifier.uri |
https://www.scopus.com/inward/record.uri?eid=2-s2.0-80053945864&doi=10.5897%2fAJPP10.156&partnerID=40&md5=93c8b9f852d11a6f1eab854bd8f3f512 |
|
dc.description.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 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. |
|
dc.subject |
alanine |
|
dc.subject |
amphotericin B |
|
dc.subject |
ellipticine |
|
dc.subject |
heterocyclic compound |
|
dc.subject |
histidine |
|
dc.subject |
isoleucine |
|
dc.subject |
leucine |
|
dc.subject |
methanol |
|
dc.subject |
methionine |
|
dc.subject |
potassium carbonate |
|
dc.subject |
resazurin |
|
dc.subject |
sterol 14alpha demethylase |
|
dc.subject |
sterol 14alpha demethylase inhibitor |
|
dc.subject |
thiadiazole derivative |
|
dc.subject |
tyrosine |
|
dc.subject |
unclassified drug |
|
dc.subject |
valine |
|
dc.subject |
voriconazole |
|
dc.subject |
animal cell |
|
dc.subject |
antifungal activity |
|
dc.subject |
article |
|
dc.subject |
binding site |
|
dc.subject |
Candida albicans |
|
dc.subject |
catalysis |
|
dc.subject |
chemical structure |
|
dc.subject |
controlled study |
|
dc.subject |
crystal structure |
|
dc.subject |
drug activity |
|
dc.subject |
drug cytotoxicity |
|
dc.subject |
drug structure |
|
dc.subject |
drug synthesis |
|
dc.subject |
enzyme active site |
|
dc.subject |
hydrophobicity |
|
dc.subject |
IC 50 |
|
dc.subject |
in vitro study |
|
dc.subject |
infrared spectroscopy |
|
dc.subject |
mass spectrometry |
|
dc.subject |
molecular docking |
|
dc.subject |
nonhuman |
|
dc.subject |
nucleophilicity |
|
dc.subject |
room temperature |
|
dc.title |
Antifungal, cytotoxic activities and docking studies of 2,5-dimercapto-1,3,4-thiadiazole derivatives |
|
dc.type |
Article |
|
dc.rights.holder |
Scopus |
|
dc.identifier.bibliograpycitation |
African Journal of Pharmacy and Pharmacology. Vol 5, No.4 (2011), p.477-485 |
|
dc.identifier.doi |
10.5897/AJPP10.156 |
|