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Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule
- Source :
- Bioorganicmedicinal chemistry letters. 23(2)
- Publication Year :
- 2012
-
Abstract
- This Letter describes the continued optimization of an MLPCN probe molecule (ML137) with a focused effort on the replacement/modification of the isatin moiety present in this highly selective M(1) PAM. A diverse range of structures were validated as viable replacements for the isatin, many of which engendered sizeable improvements in their ability to enhance the potency and efficacy of acetylcholine when compared to ML137. Muscarinic receptor subtype selectivity for the M(1) receptor was also maintained.
- Subjects :
- Isatin
Monoamine Oxidase Inhibitors
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Subtype selectivity
Biochemistry
Article
chemistry.chemical_compound
Inhibitory Concentration 50
Drug Discovery
Muscarinic acetylcholine receptor
medicine
Moiety
Molecule
Molecular Biology
Molecular Structure
Organic Chemistry
Receptor, Muscarinic M1
Muscarinic acetylcholine receptor M1
Highly selective
chemistry
Molecular Probes
Molecular Medicine
Acetylcholine
medicine.drug
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 23
- Issue :
- 2
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....f60ebe8390dd47e91fc753835d87fc8b