Syntheses of O-methylasparvenone-derived serotonin-receptor antagonists

被引：14

作者：

Bös, M ^{[1
]}

Stadler, H ^{[1
]}

Wichmann, J ^{[1
]}

Jenck, F ^{[1
]}

Martin, JR ^{[1
]}

Moreau, JL ^{[1
]}

Sleight, AJ ^{[1
]}

机构：

[1] F Hoffmann La Roche & Co Ltd, Div Pharma, Preclin CNS Res, CH-4070 Basel, Switzerland

来源：

HELVETICA CHIMICA ACTA | 1998年 / 81卷 / 03期

关键词：

D O I：

10.1002/hlca.19980810306

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Based on O-methylasparvenone (I), a N-free 5HT(2C) antagonist with moderate affinity (pK(i) = 6.7), derivatives bearing dimethylamino (7), (dimethylamino)methyl (17, 18, 21, and 22), and aminomethyl substituents (26) in place of the benzylic OH group of 1 as well as pyrrolidine- (33) and piperidine-fused derivatives (29, 43, and 45) were synthesized. In contrast to the lead structure 1, these new ligands were active in vivo in the rat. The tricycles 33 and 45 display high affinities for the 5HT(2C) receptor (pK(i) = 8).

引用

页码：525 / 538

页数：14

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