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 A2A 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
Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents / Gjorgieva Ackova, Darinka; Kotur-Stevuljevic, Jelena; Bhushan Mishra, Chandra; Mehta Luthra, Pratibha; Saso, Luciano. - In: APPLIED SCIENCES. - ISSN 2076-3417. - 9:1(2018). [10.3390/app9010113]
Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents
Luciano Saso
2018
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 A2A 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 activityI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.