296280-56-3Relevant academic research and scientific papers
Design and synthesis of naphthalenic dimers as selective MT1 melatoninergic ligands
Descamps-Fran?ois, Carole,Yous, Sa?d,Chavatte, Philippe,Audinot, Valérie,Bonnaud, Anne,Boutin, Jean A.,Delagrange, Philippe,Bennejean, Caroline,Renard, Pierre,Lesieur, Daniel
, p. 1127 - 1129 (2003)
We report the synthesis and binding properties at MT1 and MT2 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 MT1-selective ligands. The most selective one (5) behaves as an antagonist.
N-acetyl-5-arylalkoxytryptamine analogs: Probing the melatonin receptors for MT1-selectivity
Markl, Christian,Clafshenkel, William P.,Attia, Mohamed I.,Sethi, Shalini,Witt-Enderby, Paula A.,Zlotos, Darius P.
body text, p. 666 - 674 (2012/06/17)
A series of melatonin analogs obtained by the replacement of the ether methyl group with larger arylalkyl and aryloxyalkyl substituents was prepared in order to probe the melatonin receptors for MT1-selectivity. The most MT1-selective agents 11 and 15 were substituted with a Ph(CH 2)3 or a PhO(CH2)3 group. Compounds 11 and 15 displayed 11.5-fold and 11-fold higher affinity for the MT1 receptors than for the MT2 subtype. Interestingly, in our binding assay 11 and 15 have shown considerably higher MT1-affinity and selectivity than the reference ligand, the dimeric agomelatine 1a. The synthesis and pharmacological evaluation of a novel series of MLT analogs obtained by replacing the ether methyl group with arylalkyl and aryloxyalkyl moieties is described here. The results indicate for compounds 11 and 15 considerably higher MT1-affinity and selectivity than the reference ligand, the dimeric agomelatine 1a. Copyright
Substituted dimeric compounds
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, (2008/06/13)
The invention relates to compounds of formula (I): A—G1—Cy—G2—Cy—G3—B??(I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2or NR2R3, G1and G3represent an optionally substituted alkylene chain, Cy represents a ring structure and G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.
