journal article·2018-12-29Open access

Antioxidant Properties of Synthesized Bicyclic Thiazolopyrimidine Derivatives as Possible Therapeutic Agents

Darinka Gjorgieva Ackova, Jelena Kotur-Stevuljevic, Chandra Bhushan Mishra, Pratibha Mehta Luthra, Luciano Saso

Applied Sciences· Volume 9· Issue 1

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 activity.
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Research context

OpenAlex topics: Synthesis and biological activity · Synthesis and Characterization of Heterocyclic Compounds · Chemical synthesis and pharmacological studies

SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.

Affiliations

Department of Pharmacy, Faculty of Medical Sciences, University Goce Delčev-Štip, R. Krste Misirkov No. 10-A, POB 201, 2000 Štip, Macedonia

Department for Medical Biochemistry, Faculty of Pharmacy, University of Belgrade, Studentski trg 1, 11000 Belgrade, Serbia

Neuropharmaceutical Laboratory Dr. BR Ambedkar Center for Biomedical Research University of Delhi, Delhi 110007, India

Department of Physiology and Pharmacology “Vittorio Erspamer”, Sapienza University of Rome, str. Aldo Moro 5, 00185 Rome, Italy

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