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Synthesis and structure-activity relationships of novel naphthalenic and bioisosteric related amidic derivatives as melatonin receptor ligands.

Abstract：

:A series of N-naphthylethyl amide derivatives were synthesized and evaluated as melatonin receptor ligands. The affinity of each compound for the melatonin receptor was determined by binding studies using [2-125I]iodomelatonin on ovine pars tuberalis membrane homogenates. Structure-activity relationships led to the conclusion that naphthalene is a bioisostere of the indole moiety of melatonin. Moreover it appears that the affinity is strongly affected by the size of the substituent of the nitrogen of the amidic function. Many of these ligands give biphasic dose-response curves which suggests that there may be two melatonin receptor subtypes within the ovine pars tuberalis cells. The replacement of naphthalene by benzofuran or benzothiophene did not strongly alter the affinity for the melatonin receptor. In contrast, the benzimidazole analogue was a poor ligand. Compound 7, the naphthalenic analogue of melatonin, a selective ligand of the melatonin receptor and an agonist derivative, has been selected for clinical development.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Depreux P,Lesieur D,Mansour HA,Morgan P,Howell HE,Renard P,Caignard DH,Pfeiffer B,Delagrange P,Guardiola B

doi

10.1021/jm00046a006

subject

Has Abstract,Author List Incomplete

pub_date

1994-09-30 00:00:00

pages

3231-9

issue

20

eissn

0022-2623

issn

1520-4804

journal_volume

37

pub_type

杂志文章

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