SYNTHESIS, BIOLOGICAL-ACTIVITY AND ELECTROSTATIC PROPERTIES OF 3-[2-(DIMETHYLAMINO)ETHYL]-5-[(3-AMINO-1,2,4-THIADIAZOL-5-YL)METHYL]-1H-INDOLE, A NOVEL 5-HT1D RECEPTOR AGONIST

被引:10
作者
CASTRO, JL [1 ]
MATASSA, VG [1 ]
BROUGHTON, HB [1 ]
MOSLEY, RT [1 ]
STREET, LJ [1 ]
BAKER, R [1 ]
机构
[1] MERCK SHARP & DOHME LTD,DEPT MOLEC SYST,RAHWAY,NJ 07065
关键词
D O I
10.1016/S0960-894X(00)80274-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis, biological activity and electrostatic properties of the thiadiazolyl-tryptamine (2), a novel 5-HT1D receptor agonist, are described. The compound was synthesised in four steps from the readily available tryptamine ester (7c) and it was found to be remarkably more potent than the corresponding oxadiazole analogue (1), both in functional and binding assays.
引用
收藏
页码:993 / 997
页数:5
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