Synthetic approaches to bridgehead nitrogen methanesulfonamide derivatives of 3-amino-2-thioxo-2,3-dihydrothieno[2,3-d]pyrimidin-4(1H)-ones, potential cox-2 selective inhibitors
✍ Scribed by Giuseppe Granata; Salvatore Barbagallo; Antonio Perdicaro; Agostino Marrazzo; Andrea Santagati; Laura Lombardo; Venera Cardile
- Publisher
- Journal of Heterocyclic Chemistry
- Year
- 2006
- Tongue
- English
- Weight
- 162 KB
- Volume
- 43
- Category
- Article
- ISSN
- 0022-152X
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✦ Synopsis
Abstract
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Methane sulfonamide derivatives of 3‐amino‐2‐thioxo‐2,3‐dihydrothieno[2,3‐d]pyimidin‐4(1__H__)‐one, potential selective COX‐2 inhibitors, were synthesized and their structural elucidation is here reported. Some derivatives, at 10 μM concentration, showed a significant percentage of inhibition in some in vitro experiments.
📜 SIMILAR VOLUMES
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Synthesis of Functionalized 2,3-Dihydrothieno[2,3-d ]pyrimidin-4(1H )ones and Their Recyclization to 2,3-Dihydrothieno[3,4-d ]pyrimidin-4(1H )-ones
## Abstract Bridgehead nitrogen heterocycles **3a**, **b** and **6a**, **b** containing the thieno‐pyrimidine system have been prepared from the versatile intermediates 3‐amino‐2,3‐dihydro‐5,6‐dimethyl‐2‐thioxo‐thieno[2,3‐__d__]pyrimidin‐4‐(1__H__)‐one **1** and its hydrazinium or potassium salts *