N1-benzenesulfonylgramine and N1-benzenesulfonylskatole:: Novel 5-HT6 receptor ligand templates

被引：29

作者：

Pullagurla, MR

Dukat, M

Setola, V

Roth, B

Glennon, RA

机构：

[1] Virginia Commonwealth Univ, Sch Pharm, Dept Med Chem, Richmond, VA 23298 USA

[2] Case Western Reserve Univ, Dept Biochem, Cleveland, OH 44106 USA

[3] Case Western Reserve Univ, Sch Med, Dept Psychiat, Cleveland, OH 44106 USA

[4] Case Western Reserve Univ, Sch Med, Dept Neurosci, Cleveland, OH 44106 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(03)00612-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

1-Benzenesulfonyl-5-methoxy-N,N-dimethyltryptamine (3; K-i=2.3 nM) is a 5-HT6 receptor antagonist: removal of the 5-methoxy group (i.e., 6; K-i = 4.1 nM) has little impact on receptor affinity. In the present study, it is shown that the aminomethyl portion of 6 can be shortened to gramine analogue 10a (K-i = 3.1 nM) a related skatole derivative 11b (K-i = 12 nM) also binds with high affinity indicating that the aminoethyl portion of the tryptamines is not required Cor binding. Compounds 10a and 11b represent members of novel classes of 5-HT6 antagonists. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：3355 / 3359

页数：5

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