Synthesis of 4-N, N-dialkylaminoethyl-2-indolones as potential dopamine agonists

A Namil, M Benoit-Guyod, G Leclerc

文献索引：Namil, A.; Benoit-Guyod, M.; Leclerc, G. European Journal of Medicinal Chemistry, 1995 , vol. 30, # 12 p. 973 - 982

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被引用次数: 6

摘要

A set of fourteen 4-{2-[N-propyl-N-alkyl-(or alkylaryl-) amino] ethyl}-2-indolone analogues of dopamine were synthesized in 15 steps and evaluated for their affinities towards the D2 receptor using [3H] sulpiride or [3H] spiperone as radioligands. Six analogues displayed D2 agonist activities comparable (Ki= 450–650 nM) to Ropinirole or SK&F 101468. The functionalized amino side chain introduced in the 4-position can be used to modulate the ...