Design and synthesis of 3-alkyl-2-aryl-1,3-thiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors |
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| Authors: | Tannaz Zebardast Afshin Zarghi Bahram Daraie Mehdi Hedayati Orkideh G. Dadrass |
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| Affiliation: | 1. Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University (M.C), Tehran, Iran;2. Pharmaceutical Research Center, School of Pharmacy, Shahid Beheshti University (M.C), Tehran, Iran;3. Department of Toxicology, Tarbiat Modarres University, Tehran, Iran;4. Endocrine Research Center, Shahid Beheshti University (M.C), Tehran, Iran;5. Department of Pharmaceutical Chemistry, School of Pharmacy, Azad University, Tehran, Iran |
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| Abstract: | A new group of 3-alkyl-2-aryl-1,3-thiazinan-4-ones, possessing a methylsulfonyl pharmacophore, were synthesized and their biological activities were evaluated for cyclooxygenase-2 (COX-2) inhibitory activity. In vitro COX-1/COX-2 inhibition studies identified 3-benzyl-2-(4-methylsulfonylphenyl)-1,3-thiazinan-4-one (11a) as a potent (IC50 = 0.06 μM) and selective (selectivity index >285) COX-2 inhibitor. |
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