Publication:
Antifungal, cytotoxic activities and docking studies of 2,5-dimercapto-1,3,4-thiadiazole derivatives

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Issued Date

2011

Resource Type

Article

File Type

application/pdf

ISSN

19960816

DOI

10.5897/AJPP10.156

Other identifier(s)

2-s2.0-80053945864

Rights Holder(s)

มหาวิทยาลัยศรีนครินทรวิโรฒ

Bibliographic Citation

African Journal of Pharmacy and Pharmacology. Vol 5, No.4 (2011), p.477-485

Suggested Citation

Samee W., Vajragupta O. 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), p.477-485. doi:10.5897/AJPP10.156 Retrieved from: https://hdl.handle.net/20.500.14740/7420

Title

Antifungal, cytotoxic activities and docking studies of 2,5-dimercapto-1,3,4-thiadiazole derivatives

Author(s)

Samee W.
 Vajragupta O.

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.

Subject(s)

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

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URI

https://hdl.handle.net/20.500.14740/7420

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Scopus: Year 1983-2021

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