Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.
Article Details
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Starck JP, Talaga P, Quere L, Collart P, Christophe B, Lo Brutto P, Jadot S, Chimmanamada D, Zanda M, Wagner A, Mioskowski C, Massingham R, Guyaux M
Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.
Bioorg Med Chem Lett. 2006 Jan 15;16(2):373-7. Epub 2005 Nov 3.
- PubMed ID
- 16275087 [ View in PubMed]
- Abstract
The synthesis and biological evaluation of a novel family of M(3) muscarinic antagonists are described. A systematic modification of the substituents to a novel alkyne-quinuclidine scaffold yielded original compounds displaying potent in vitro anticholinergic properties.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Darifenacin Muscarinic acetylcholine receptor M2 Ki (nM) 50 N/A N/A Details Darifenacin Muscarinic acetylcholine receptor M3 Ki (nM) 1.3 N/A N/A Details Oxybutynin Muscarinic acetylcholine receptor M2 Ki (nM) 16 N/A N/A Details Oxybutynin Muscarinic acetylcholine receptor M3 Ki (nM) 1.3 N/A N/A Details Tolterodine Muscarinic acetylcholine receptor M2 Ki (nM) 4 N/A N/A Details Tolterodine Muscarinic acetylcholine receptor M3 Ki (nM) 3.2 N/A N/A Details