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Synthesis of 5-substituted-2,3-dihydro-1,4-benzoxathiins: biological evaluation as melatonin receptors ligands
Authors:Charton Isabelle  Suzenet Franck  Boutin Jean A  Audinot Valérie  Delagrange Philippe  Bennejean Caroline  Renard Pierre  Guillaumet Gérald
Institution:Institut de Chimie Organique et Analytique, UMR-CNRS 6005, Université d'Orléans, rue de Chartres, BP 6759, 45067 Orléans Cedex 02, France.
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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