Synthesis and receptor activity of 2-substituted 8-methyl-5-(2-pyridinylethyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles
A series of new 2-substituted 8-methyl-5-(2-pyridinylethyl)-2,3,4,5-tetrahydro-1 H -pyrido[4,3- b ]indoles have been synthesized. Their activity profiles were studied on a broad panel of therapeutic targets including GPC-receptors, ion channels, and neurotransmitter transporters. One of the studied...
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Veröffentlicht in: | Pharmaceutical chemistry journal 2013-04, Vol.47 (1), p.12-19 |
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Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | A series of new 2-substituted 8-methyl-5-(2-pyridinylethyl)-2,3,4,5-tetrahydro-1
H
-pyrido[4,3-
b
]indoles have been synthesized. Their activity profiles were studied on a broad panel of therapeutic targets including GPC-receptors, ion channels, and neurotransmitter transporters. One of the studied compounds, 2-methyl-3-{2-[8-methyl-5-(2-pyridin-2-ylethyl)-2,3,4,5-tetrahydropyridino[4,3-
b
]indol-2-yl]ethyl}-6,7,8,9-tetrahydropyrido[1,2-
a
]pyrimidin-4-one, was found to be a highly active antagonist of adrenergic α
1A
, α
1B
, α
1D
, and α
2A
receptors and serotonin 5-HT
2A
, 5-HT
2B
, 5-HT
2C
, and 5-HT
7
receptors. The results were considered in terms of structure—activity relationships. It was established that introduction of bulky substituents into the 2-position of the other synthesized 8-methyl-5-(2-pyridinylethyl)-2,3,4,5-tetrahydro-1
H
-pyrido[4,3-
b
]indoles led to an activity decrease of the corresponding derivatives as compared with that of the 2,8-dimethyl analogs. |
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ISSN: | 0091-150X 1573-9031 |
DOI: | 10.1007/s11094-013-0887-4 |