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In vitro antioxidant activity of thiazolidinone derivatives of 1,3-thiazole and 1,3,4-thiadiazole

Authorized Users Only
2018
Authors
Đukić, Mirjana
Fesatidou, Mara
Xenikakis, Iakovos
Geronikaki, Athina
Angelova, Violina T.
Savić, Vladimir
Pasić, Marta
Krilović, Branislav
Đukić, Dušan
Gobeljić, Borko
Pavlica, Marina
Đurić, Ana
Stanojević, Ivan
Vojvodić, Danilo
Saso, Luciano
Article (Published version)
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Abstract
The initial steps in preclinical drug developing research concern the synthesis of new compounds for specific therapeutic use which needs to be confirmed by in vitro and then in vivo testing. Nine thiazolidinone derivatives (numerically labeled 1-9) classified as follows: 1,3-thiazole-based compounds (1 and 2); 1,3,4-thiadiazole based compounds (3 and 4); substituted 5-benzylideno-2-adamantylthiazol[3,2-b] [1,2,4] triazol-6(5H) ones (5-8); and an ethylaminothiazole-based chalcone (9), were tested for antioxidant activity (AOA) by using three in vitro assays: DPPH (1,1-diphenyl-2-picrylhydrazyl scavenging capacity test); FRAP (ferric reducing antioxidant power test); and TBARS (thiobarbituric acid reactive substances test). Compounds 1-4 and 9 in particular are newly synthesized compounds. Also, traditional antioxidants Vitamins E and C and alpha-lipoic acid (alpha-LA) were tested. The results of DPPH testing: Vitamin C 94.35%, Vitamin E 2.99% and alpha-LA 1.57%; compounds: 4 33.98%; 2 ...18.73%; 1 15.62%; 5 6.59%; 3 4.99%; 6-9 demonstrated almost no AOA. The results of TBARS testing (% of LPO inhibition): Vitamin C 62.32%; Vitamin E 36.29%; alpha-LA 51.36%; compounds: 1 62.11%; 5 66.71%; 9 60.93%; 4, 6 and 7 demonstrated similar to 50%; 3 and 8 displayed similar to 38%; 2 23.51%. By FRAP method, Vitamins E and C showed equal AOA, similar to 100%, unlike alpha-LA (no AOA), and AOA of the tested compounds (expressed as a fraction of the AOA of Vitamin C) were: 2 and 4-75%; 8, 3 and 1-45%; 5-7 and 9-27%. Different red-ox reaction principles between these assays dictate different AOA outcomes for a single compound. Vitamin C appeared to be the superior antioxidant out of the traditional antioxidants; and compound 4 was superior to other tested thiazolidinone derivatives. Vitamin C appeared to be the superior antioxidant out of the traditional antioxidants; and compound 4 was superior to other tested thiazolidinone derivatives. Phenyl-functionalized benzylidene, amino-carbonyl functional domains and chelating ligand properties of the thiazolidinone derivatives correlated with AOA.

Keywords:
1,3-thiazole, 1,3,4-thiadiazole / Thiazolidinone / DPPH / FRAP / TBARS
Source:
Chemico-Biological Interactions, 2018, 286, 119-131
Publisher:
  • Elsevier Ireland Ltd, Clare
Projects:
  • Preventive, therapeutic, and ethical approach in preclinical and clinical studies of the genes and modulators of redox cell signaling in immune, inflammatory and proliferative cell response (RS-41018)

DOI: 10.1016/j.cbi.2018.03.013

ISSN: 0009-2797

PubMed: 29574026

WoS: 000429592200015

Scopus: 2-s2.0-85044467819
[ Google Scholar ]
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19
URI
http://farfar.pharmacy.bg.ac.rs/handle/123456789/3154
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  • Radovi istraživača / Researchers’ publications
Institution
Pharmacy

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