Synthesis of N1-Phenethyl Substituted Indole Derivatives as New Melatoninergic Agonists and Antagonists

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The potency of new indolic N1-phenethyl substituted melatoninergic ligands with and without methyl groups in the α and β position of the alkanamidoethyl side chain was examined using the pigment aggregation response in a clonal line of Xenopus laevis melanophores. The non 5-OMe substituted compounds, 8a-e, are all weak antagonists while introduction of the 5-OMe group, 9a-e, increases both agonist and antagonist activity except for 9c(R=C_3H_7), which is only an agonist and 9e(R=c-C_4H_7), which is only an antagonist. Introduction of an α-methyl group into the 5-OMe derivatives, 14a-e, reduces the agonist potency while introduction of a β-methyl group has only a small effect on either the agonist or antagonist potency. Double β-methyl substitution of the 5-OMe derivatives, 20a-e, generally increases the agonist potential(20c, R=C_3H_7 is the most potent agonist of the compounds described)and decreases the antagonist potency, except for 20a(R=CH_3), which is the most potent antagonist of this series of compounds.
公益社団法人日本薬学会の論文
2002-01-01