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Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012
- Source :
- Bioorganicmedicinal chemistry letters. 22(15)
- Publication Year :
- 2012
-
Abstract
- This Paper describes the continued optimization of an MLPCN probe molecule M(1) antagonist (ML012) through an iterative parallel synthesis approach. After several rounds of modifications of the parent compound, we arrived at a new azetidine scaffold that displayed improved potency while maintaining a desirable level of selectivity over other muscarinic receptor subtypes. Data for representative molecules 7w (VU0452865) and 12a (VU0455691) are presented.
- Subjects :
- Stereochemistry
Clinical Biochemistry
Azetidine
Pharmaceutical Science
Biochemistry
Article
chemistry.chemical_compound
Structure-Activity Relationship
Thiadiazoles
Cytochrome P-450 Enzyme System
Drug Discovery
Structure–activity relationship
Animals
Humans
Protein Isoforms
Molecular Biology
Sulfonamides
Extramural
Chemistry
Organic Chemistry
Receptor, Muscarinic M1
Antagonist
Rats
Molecular Probes
Molecular Medicine
Azetidines
Molecular probe
Azabicyclo Compounds
Protein Binding
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 22
- Issue :
- 15
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....8a85b9b4efc2c8a3565c032688fcbd69