Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents
2019
Аутори
Gjorgieva-Ackova, DarinkaKotur-Stevuljević, Jelena
Mishra, Chandra Bhushan
Luthra, Pratibha Mehta
Saso, Luciano
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
Oxidant/antioxidant imbalance in the body has been implicated as one of the pathophysiological mechanisms leading to disease development. Therefore, we searched for a good antioxidant candidate that can be used as a therapeutic agent alone or in combination with other reported drugs. Earlier, we reported the A(2A) receptor antagonist properties of 7-Imino-3-substituted-2-thioxo-3,7-dihydro-2H-thiazolo[4,5-d]pyrimidin-6-yl)-urea derivatives (compounds 1-12) and the neuroprotective effect of compound 2. Therefore, in the present work, the antioxidant potential of compounds 1-12 was studied. Compounds 1-12 were screened using different (red/ox) tests, such as the Ferric Reducing Antioxidant Power (FRAP) assay, to determine total antioxidant activity, redox status tests (with and without prooxidants) such as Advanced Oxidation Protein Products (AOPP) and Total Oxidative Status (TOS) which measures H2O2 and lipid hydroperoxides, Paraoxonase-1 Enzyme Activity (PON1), Total SH-groups content,... and Total Antioxidative Status (TAS) for antioxidant determination. The Prooxidative Score, Antioxidative Score, and Oxy Score were also calculated. From the obtained results, compounds 6 (8720 FRAP value and 39.31 Oxy Score) and 12 (7866 FRAP value and 36.41 Oxy Score) were found to possess significant antioxidant activity with reasonable potential for therapeutic activity.
Кључне речи:
thiazolopyrimidine derivatives / reactive oxygen species / antioxidant potential / redox-testsИзвор:
Applied Sciences, Basel, 2019, 9, 1Издавач:
- MDPI, Basel
DOI: 10.3390/app9010113
ISSN: 2076-3417
WoS: 000456579300113
Scopus: 2-s2.0-85059345097
Институција/група
PharmacyTY - JOUR AU - Gjorgieva-Ackova, Darinka AU - Kotur-Stevuljević, Jelena AU - Mishra, Chandra Bhushan AU - Luthra, Pratibha Mehta AU - Saso, Luciano PY - 2019 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3327 AB - Oxidant/antioxidant imbalance in the body has been implicated as one of the pathophysiological mechanisms leading to disease development. Therefore, we searched for a good antioxidant candidate that can be used as a therapeutic agent alone or in combination with other reported drugs. Earlier, we reported the A(2A) receptor antagonist properties of 7-Imino-3-substituted-2-thioxo-3,7-dihydro-2H-thiazolo[4,5-d]pyrimidin-6-yl)-urea derivatives (compounds 1-12) and the neuroprotective effect of compound 2. Therefore, in the present work, the antioxidant potential of compounds 1-12 was studied. Compounds 1-12 were screened using different (red/ox) tests, such as the Ferric Reducing Antioxidant Power (FRAP) assay, to determine total antioxidant activity, redox status tests (with and without prooxidants) such as Advanced Oxidation Protein Products (AOPP) and Total Oxidative Status (TOS) which measures H2O2 and lipid hydroperoxides, Paraoxonase-1 Enzyme Activity (PON1), Total SH-groups content, and Total Antioxidative Status (TAS) for antioxidant determination. The Prooxidative Score, Antioxidative Score, and Oxy Score were also calculated. From the obtained results, compounds 6 (8720 FRAP value and 39.31 Oxy Score) and 12 (7866 FRAP value and 36.41 Oxy Score) were found to possess significant antioxidant activity with reasonable potential for therapeutic activity. PB - MDPI, Basel T2 - Applied Sciences, Basel T1 - Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents VL - 9 IS - 1 DO - 10.3390/app9010113 ER -
@article{ author = "Gjorgieva-Ackova, Darinka and Kotur-Stevuljević, Jelena and Mishra, Chandra Bhushan and Luthra, Pratibha Mehta and Saso, Luciano", year = "2019", abstract = "Oxidant/antioxidant imbalance in the body has been implicated as one of the pathophysiological mechanisms leading to disease development. Therefore, we searched for a good antioxidant candidate that can be used as a therapeutic agent alone or in combination with other reported drugs. Earlier, we reported the A(2A) receptor antagonist properties of 7-Imino-3-substituted-2-thioxo-3,7-dihydro-2H-thiazolo[4,5-d]pyrimidin-6-yl)-urea derivatives (compounds 1-12) and the neuroprotective effect of compound 2. Therefore, in the present work, the antioxidant potential of compounds 1-12 was studied. Compounds 1-12 were screened using different (red/ox) tests, such as the Ferric Reducing Antioxidant Power (FRAP) assay, to determine total antioxidant activity, redox status tests (with and without prooxidants) such as Advanced Oxidation Protein Products (AOPP) and Total Oxidative Status (TOS) which measures H2O2 and lipid hydroperoxides, Paraoxonase-1 Enzyme Activity (PON1), Total SH-groups content, and Total Antioxidative Status (TAS) for antioxidant determination. The Prooxidative Score, Antioxidative Score, and Oxy Score were also calculated. From the obtained results, compounds 6 (8720 FRAP value and 39.31 Oxy Score) and 12 (7866 FRAP value and 36.41 Oxy Score) were found to possess significant antioxidant activity with reasonable potential for therapeutic activity.", publisher = "MDPI, Basel", journal = "Applied Sciences, Basel", title = "Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents", volume = "9", number = "1", doi = "10.3390/app9010113" }
Gjorgieva-Ackova, D., Kotur-Stevuljević, J., Mishra, C. B., Luthra, P. M.,& Saso, L.. (2019). Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents. in Applied Sciences, Basel MDPI, Basel., 9(1). https://doi.org/10.3390/app9010113
Gjorgieva-Ackova D, Kotur-Stevuljević J, Mishra CB, Luthra PM, Saso L. Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents. in Applied Sciences, Basel. 2019;9(1). doi:10.3390/app9010113 .
Gjorgieva-Ackova, Darinka, Kotur-Stevuljević, Jelena, Mishra, Chandra Bhushan, Luthra, Pratibha Mehta, Saso, Luciano, "Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents" in Applied Sciences, Basel, 9, no. 1 (2019), https://doi.org/10.3390/app9010113 . .