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Synthesis and preliminary pharmacological results on new naphthalene derivatives as 5-HT(4) receptor ligands.
Diouf O, Depreux P, Chavatte P, Poupaert JH
Institut de chimie pharmaceutique Albert Lespagnol, 3, rue du Professeur Laguesse, BP 83, 59006 cedex, Lille, France.
The indole derivative GR 113808 is currently used as the reference ligand for labelling the 5-HT(4) serotoninergic receptors. Previous works in our laboratories established the bioisosteric equivalency of the indole heterocycle and naphthalene in a series of melatonin receptor ligands. Based on this knowledge we designed new analogues of GR 113808 by introducing two bioisosteric modifications: firstly, the indole ring was replaced by a naphthalene one and secondly, the ester linkage was replaced by an amide group. Compound 8 emerged within this novel series as it displayed high and selective affinity at 5-HT(4) receptors (Ki 5-HT(4) = 6 nM, Ki 5-HT(3) = 100 nM, Ki values at other 5-HT receptors were higher than 1000 nM). Compound 8 is currently undergoing further pharmacological evaluation.
PMID: 10960185, UI: 20416438
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