Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors

被引：28

作者：

Bauer, Udo ^{[1
]}

Giordanetto, Fabrizio ^{[1
]}

Bauer, Martin ^{[1
]}

O'Mahony, Gavin ^{[1
]}

Johansson, Kjell E. ^{[1
]}

Knecht, Wolfgang ^{[1
]}

Hartleib-Geschwindner, Judith ^{[1
]}

Carlsson, Eva Toppner ^{[1
]}

Enroth, Cristofer ^{[2
]}

机构：

[1] AstraZeneca, R&D Molndal, S-43183 Molndal, Sweden

[2] Katedralskolan, Dept Nat Sci, S-53288 Skara, Sweden

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 05期

关键词：

PDE10A; Phosphodiesterase; Hit to lead; Enzyme inhibitor; Naphthyridine; DIHYDROOROTATE DEHYDROGENASE;

D O I：

10.1016/j.bmcl.2012.01.046

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1,6-naphthyridine-based compounds was synthesized as potent phosphodiesterase 10A (PDE10A) inhibitors. Structure-based chemical modifications of the discovered chemotype served to further improve potency and selectivity over DHODH, laying the foundation for future optimization efforts. (c) 2012 Elsevier Ltd. All rights reserved.

引用

页码：1944 / 1948

页数：5

共 17 条

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