Synthesis and Structure Activity Relationship of Rigidized Indolyl Pyrrolidine Derivatives as 5-HT6 Receptor Ligands

被引：1

作者：

Nirogi, Ramakrishna ^{[1
]}

Dwarampudi, Adireddy ^{[1
,2
]}

Bhatta, Venugopalarao ^{[1
]}

Kota, Laxman ^{[1
]}

Dubey, P. K. ^{[2
]}

机构：

[1] Suven Life Sci Ltd, Discovery Res, Hyderabad 500034, Andhra Pradesh, India

[2] Jawaharlal Nehru Technol Univ Hyderabad, Dept Chem, Hyderabad 500085, Andhra Pradesh, India

来源：

ASIAN JOURNAL OF CHEMISTRY | 2013年 / 25卷 / 16期

关键词：

5-HT6R; Structure activity relationship; Pharmacokinetic; Brain penetration; Water maze; Cognition;

D O I：

10.14233/ajchem.2013.15443

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A novel series of rigidized indolyl pyrrolidine derivatives have been designed by constraining the tryptamine nitrogen through alpha and beta carbons. All the synthesized derivatives have shown moderate affinities at 5-HT6R when tested in in vitro binding assay. Synthesis, structure activity relationship (SAR), pharmacokinetic profile and in vivo efficacy of a selected compound is the subject matter of this communication.

引用

页码：9293 / 9298

页数：6

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