Synthesis and preliminary pharmacological results on new naphthalene derivatives as 5-HT4 receptor ligands
(2000) European Journal of Medicinal Chemistry — Vol. 35, n° 7-8, p. 699-706 (2000)
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- Abstract
- The indole derivative GR 113808 is currently used as the reference Ligand for labelling the 5-HT4 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-HT4 receptors (Ki 5-HT4 = 6 nM, Ki 5-HT3 = 100 nM, Ki values at other 5-HT receptors were higher than 1 000 nM). Compound 8 is currently undergoing further pharmacological evaluation. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
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Diouf, O., Depreux, P., Chavatte, P., & Poupaert, J. (2000). Synthesis and preliminary pharmacological results on new naphthalene derivatives as 5-HT4 receptor ligands. European Journal of Medicinal Chemistry, 35(7-8), 699-706. https://doi.org/10.1016/S0223-5234(00)00163-X (Original work published 2000)