Isabelle Charton

Université d'Orléans

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Co-Authors

Caroline Bennejean

Servier (France)

Gérald Guillaumet

Institut de Chimie Organique et Analytique

Ahmed Mamai

Ontario Institute for Cancer Research

Philippe Delagrange

Servier (France)

Peter J. Morgan

University of Aberdeen

Pierre Renard

ADIR Association

Marie‐Claude Viaud

Université d'Orléans

Béatrice Guardiola‐Lemaître

Servier (France)

H.E. Howell

University of the Free State

M.C. Viaud

Université d'Orléans

Cooperative Institutions

Centre National de la Recherche Scientifique

Institut des Hautes Études Scientifiques

Servier (France)

Université d'Orléans

Institut de Chimie Organique et Analytique

Université de Rouen Normandie

Inserm

Normandie Université

Institute for International Social Research

Différenciation et Communication Neuronale et Neuroendocrine

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Substituted oxygenated heterocycles and thio-analogues: synthesis and biological evaluation as melatonin ligands

Bioorganic & Medicinal Chemistry (2000)

Isabelle Charton Ahmed Mamai Caroline Bennejean Pierre Renard Edward H. Howell

Moiety

Thio-

10.1016/s0968-0896(99)00265-5

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Citations (15)

Synthesis of 5-Substituted-2,3-dihydro-1,4-benzoxathiins: Biological Evaluation as Melatonin Receptors Ligands

Journal of Enzyme Inhibition and Medicinal Chemistry (2003)

Isabelle Charton Franck Suzenet Jean A. Boutin Valérie Audinot Philippe Delagrange

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.

Sulfonium

10.1080/1475636032000096855

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Citations (8)

Synthesis and Biological Activity of New Melatonin Receptor Ligands

Pharmacy and Pharmacology Communications (2000)

Isabelle Charton Ahmed Mamai Caroline Bennejean Pierre‐Yves Renard Philippe Delagrange

To discover analogues of melatonin with a longer half-life, novel non-indole analogues of the compound, in which the amide group of the side-chain has been reversed, have been prepared and evaluated in binding assays to determine their activity on melatonin receptors. The two most active compounds were those with the N-methylbutyramide side-chain. Butyramide and pentanoylamide side-chains resulted in similar affinities, irrespective of the skeleton tested whereas a propionamide side-chain led to loss of affinity. The biological actity of the molecules was more influenced by the length of the side-chain than by the nature of the skeleton, which had little effect. The results obtained show the relative importance of the length of the side-chain and of the nature of the skeleton in both the binding to and the activity on the melatonin receptor of the retroamide series.

Side chain

Amide

Affinities

Skeleton (computer programming)

10.1211/146080800128735638

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Citations (11)