Synthesis and biological evaluation of new beta,beta'-disubstituted 6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl ethylamido melatoninergic ligands
| Autor: | Maria Panoussopoulou, David Sugden, Katherine Hough, Andrew Tsotinis |
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| Rok vydání: | 2003 |
| Předmět: |
Agonist
chemistry.chemical_classification Indoles Chemistry Ligand Stereochemistry medicine.drug_class Substituent Melanophores Pharmaceutical Science Biological activity Melatonin receptor Chemical synthesis Pigment granule chemistry.chemical_compound Structure-Activity Relationship Xenopus laevis Culture Techniques medicine Animals Drug Interactions Alkyl Melatonin |
| Zdroj: | European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 18(5) |
| ISSN: | 0928-0987 |
| Popis: | Tricyclic analogs of melatonin with alkyl and cycloalkyl moieties in the beta position of the ethylamido chain have been prepared and tested for their ability to activate pigment granule aggregation in Xenopus laevis melanophores. The introduction of two methyl groups in the beta position of the side-chain of the methoxyl-substituted ligands induces a synergistic effect in agonist potency, which, importantly, is maintained after the methoxyl substituent is removed. The presence of more bulky beta-substituents, regardless of the size of the R group, seems to lead to antagonism. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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