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. 1998 Sep-Oct;53(5):429-37.

[Melatonin, a pertinent prototype for therapeutic innovation]

[Article in French]
D Lesieur  1 , V Leclerc, P Chavatte, C Marot, P Renard, B Guardiola-Lemaitre
Affiliations
  • PMID: 9921034

[Melatonin, a pertinent prototype for therapeutic innovation]

[Article in French]
D Lesieur et al. Therapie. 1998 Sep-Oct.

Abstract

Melatonin fulfils most of the requirements of a typical lead compound for rational drug design. We have rationally modified each of its structural features with a view to clarifying their role in drug-receptor interactions (affinity and activity) and to obtain agonist and antagonist ligands which could be used as pharmacological tools and/or as drugs. Molecular modelling studies allow us to propose a pharmacophore model. The naphthalenic bioisostere of melatonin (agomelatin) is currently under clinical (phase II) evaluation and two other compounds have been selected for development.

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