Mild and efficient synthesis of new tetraketones as lipoxygenase inhibitors and antioxidants |
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| Authors: | Ghulam M Maharvi Samar Ali Naheed Riaz Nighat Afza Abdul Malik Muhammad Ashraf |
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| Institution: | 1. Pharmaceutical Research Centre, PCSIR Laboratories Complex, Karachi, 75280, Pakistan;2. International Centre for Chemical and Biological Sciences, H.E.J. Research Institute of Chemistry, University of Karachi, Karachi, 75270, Pakistan;3. Department of Pharmacy, Islamia University, Bahawalpur, Pakistan |
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| Abstract: | A mild and efficient route to tetraketones (2–22) has been developed by way of tetraethyl ammonium bromide (Et4N+Br? ) mediated condensation of dimedone (5,5-dimethylcyclohexane-1,3-dione, 1) with a variety of aldehydes. All these compounds showed significant lipoxygenase inhibitory activity and moderate to strong antioxidant potential. Compounds 19 (IC50 = 7.8 μM), 22 (IC50 = 12.5 μM), 3 (IC50 = 16.3 μM), 11 (IC50 = 17.5 μM) and 8 (IC50 = 21.3 μM) showed significant inhibitory potential against lipoxygenase (baicalein, IC50 = 22.4 μM). On the other hand compound 19 (IC50 = 33.6 μM) also showed strong antioxidant activity compared to the standard (IC50 = 44.7 μM). This study is likely to lead to the discovery of therapeutically efficient agents against very important disorders including inflammation, asthma, cancer and autoimmune diseases. |
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| Keywords: | Tetraketones Inhibitory activity Lipoxygenase Antioxidant |
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