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Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Aug 01; Vol. 22 (15), pp. 5035-40. Date of Electronic Publication: 2012 Jun 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.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Azabicyclo Compounds chemical synthesis
Azabicyclo Compounds metabolism
Azetidines chemical synthesis
Azetidines metabolism
Cytochrome P-450 Enzyme System metabolism
Humans
Protein Binding
Protein Isoforms antagonists & inhibitors
Protein Isoforms metabolism
Rats
Receptor, Muscarinic M1 metabolism
Structure-Activity Relationship
Azabicyclo Compounds chemistry
Azetidines chemistry
Molecular Probes chemistry
Receptor, Muscarinic M1 antagonists & inhibitors
Sulfonamides chemistry
Thiadiazoles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 15
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 22749871
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.06.018