Synthesis of 5-substituted-2,3-dihydro-1,4-benzoxathiins: biological evaluation as melatonin receptors ligands |
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Authors: | Charton Isabelle Suzenet Franck Boutin Jean A Audinot Valérie Delagrange Philippe Bennejean Caroline Renard Pierre Guillaumet Gérald |
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Affiliation: | Institut de Chimie Organique et Analytique, UMR-CNRS 6005, Université d'Orléans, rue de Chartres, BP 6759, 45067 Orléans Cedex 02, France. |
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Abstract: | The synthesis of benzoxathiins bearing a retroamide function is described from 8-hydroxythiochroman, the key step involving the synthesis of the benzoxathiin ring through a sulfonium salt. These new melatonin analogues were evaluated on human receptors MT1 and MT2 and have a similar affinity to that of melatonin itself. |
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