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Rapid access towards follow-up NOP receptor agonists using a knowledge based approach
- Source :
- Bioorganicmedicinal chemistry letters. 19(22)
- Publication Year :
- 2009
-
Abstract
- A knowledge based approach has been adopted to identify novel NOP receptor agonists with simplified hydrophobes. Substitution of the benzimidazol-2-one piperidine motif with a range of hydrophobic groups and pharmacophore guided bio-isosteric replacement of the benzimidazol-2-one moiety was explored. Compound 51 was found to be a high affinity, potent NOP receptor agonist with reduced affinity for the hERG channel.
- Subjects :
- Agonist
medicine.drug_class
Stereochemistry
Narcotic Antagonists
Clinical Biochemistry
NOP
hERG
Pharmaceutical Science
Biochemistry
Nociceptin Receptor
chemistry.chemical_compound
Structure-Activity Relationship
Piperidines
Cricetinae
Drug Discovery
Rapid access
medicine
Moiety
Animals
Receptor
Molecular Biology
biology
Organic Chemistry
chemistry
Receptors, Opioid
biology.protein
Molecular Medicine
Benzimidazoles
Piperidine
Pharmacophore
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 19
- Issue :
- 22
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....62fe4ddf63cb135568f4a115431ad52a