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
  • 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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