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Discovery, characterization and biological evaluation of a novel ( R )-4,4-difluoropiperidine scaffold as dopamine receptor 4 (D 4 R) antagonists
- Source :
- Bioorganic & Medicinal Chemistry Letters. 26:5757-5764
- Publication Year :
- 2016
- Publisher :
- Elsevier BV, 2016.
-
Abstract
- Herein, we report the synthesis and structure-activity relationship of a novel series of (R)-4,4-difluoropiperidine core scaffold as dopamine receptor 4 (D4) antagonists. A series of compounds from this scaffold are highly potent against the D4 receptor and selective against the other dopamine receptors. In addition, we were able to confirm the active isomer as the (R)-enantiomer via an X-ray crystal structure.
- Subjects :
- Scaffold
010405 organic chemistry
Stereochemistry
Chemistry
Organic Chemistry
Clinical Biochemistry
Pharmaceutical Science
01 natural sciences
Biochemistry
0104 chemical sciences
03 medical and health sciences
0302 clinical medicine
Dopamine receptor
Drug Discovery
Molecular Medicine
Receptor
Molecular Biology
030217 neurology & neurosurgery
Biological evaluation
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 26
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi...........30f8564f659d5a5117a9c3d470cb816f