Diphenylsulfone muscarinic antagonists: piperidine derivatives with high m2 selectivity and improved potency
| Autor: | Ruth A. Duffy, Sundeep Dugar, Gordon Crosby, Vilma Ruperto, Herbert Binch, Robert D. McQuade, Lian-Yong Chen, Kristen Bratzler, John W. Clader, Lisa A. Taylor, Pradeep B. Pushpavanam, Jean E. Lachowicz, William Billard |
|---|---|
| Rok vydání: | 2000 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Pharmaceutical Science Muscarinic Antagonists Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Piperidines Drug Discovery Muscarinic acetylcholine receptor medicine Animals Potency Molecular Biology Acetylcholine receptor Receptor Muscarinic M2 Molecular Structure Chemistry Organic Chemistry Receptors Muscarinic Acetylcholine Corpus Striatum Rats Piperazine Molecular Medicine Piperidine Lead compound medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 10:2209-2212 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(00)00437-6 |
| Popis: | Piperidine analogues of our previously described piperazine muscarinic antagonists are described. Piperidine analogues show a distinct structure–activity relationship (SAR) that differs from comparable piperazines. Compounds with high selectivity and improved potency for the M 2 receptor have been identified. The lead compound, 12b , increases acetylcholine release in vivo. Compounds of this class may be useful for the treatment of cognitive disorders such as Alzheimer's disease (AD). |
| Databáze: | OpenAIRE |
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