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

Bauer, Udo ; Giordanetto, Fabrizio ; Bauer, Martin ; O'Mahony, Gavin ; Johansson, Kjell E ; Knecht, Wolfgang LU ; Hartleib-Geschwindner, Judith ; Carlsson, Eva Töppner and Enroth, Cristofer (2012) In Bioorganic & Medicinal Chemistry Letters 22(5). p.1944-1948
Abstract

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.

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author
; ; ; ; ; ; ; and
publishing date
type
Contribution to journal
publication status
published
keywords
Antipsychotic Agents/chemistry, Humans, Models, Molecular, Naphthyridines/chemistry, Nitriles/chemistry, Phosphodiesterase Inhibitors/chemistry, Phosphoric Diester Hydrolases/chemistry, Structure-Activity Relationship
in
Bioorganic & Medicinal Chemistry Letters
volume
22
issue
5
pages
1944 - 1948
publisher
Elsevier
external identifiers
  • scopus:84857355907
  • pmid:22321214
ISSN
0960-894X
DOI
10.1016/j.bmcl.2012.01.046
language
English
LU publication?
no
id
6f2b2247-f25f-466f-8150-f906c21e17fd
date added to LUP
2020-07-17 14:10:24
date last changed
2024-05-01 15:05:31
@article{6f2b2247-f25f-466f-8150-f906c21e17fd,
  abstract     = {{<p>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.</p>}},
  author       = {{Bauer, Udo and Giordanetto, Fabrizio and Bauer, Martin and O'Mahony, Gavin and Johansson, Kjell E and Knecht, Wolfgang and Hartleib-Geschwindner, Judith and Carlsson, Eva Töppner and Enroth, Cristofer}},
  issn         = {{0960-894X}},
  keywords     = {{Antipsychotic Agents/chemistry; Humans; Models, Molecular; Naphthyridines/chemistry; Nitriles/chemistry; Phosphodiesterase Inhibitors/chemistry; Phosphoric Diester Hydrolases/chemistry; Structure-Activity Relationship}},
  language     = {{eng}},
  month        = {{03}},
  number       = {{5}},
  pages        = {{1944--1948}},
  publisher    = {{Elsevier}},
  series       = {{Bioorganic & Medicinal Chemistry Letters}},
  title        = {{Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors}},
  url          = {{http://dx.doi.org/10.1016/j.bmcl.2012.01.046}},
  doi          = {{10.1016/j.bmcl.2012.01.046}},
  volume       = {{22}},
  year         = {{2012}},
}