2. Academic Validation
  3. Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands

Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands

  • J Med Chem. 2003 Mar 27;46(7):1127-9. doi: 10.1021/jm0255872.
Carole Descamps-François 1,  Saïd Yous,  Philippe Chavatte,  Valérie Audinot,  Anne Bonnaud,  Jean A Boutin,  Philippe Delagrange,  Caroline Bennejean,  Pierre Renard,  Daniel Lesieur
Affiliations

Affiliation

  • 1 Faculté de Pharmacie, Laboratoire de Chimie Thérapeutique, Université de Lille 2, 3 Rue du Professeur Laguesse, BP 83, 59006 Lille Cedex, France.
PMID: 12646022 DOI: 10.1021/jm0255872
Abstract

We report the synthesis and binding properties at MT(1) and MT(2) receptors of the first example of agomelatine (N-[2-(7-methoxynaphth-1-yl)ethyl]acetamide) dimers in which two agomelatine moieties are linked together through their methoxy substituent by a polymethylene side chain according to the "bivalent ligand" approach. Some of these compounds behave as MT(1)-selective ligands. The most selective one (5) behaves as an antagonist.

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