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Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Jun 01; Vol. 21 (11), pp. 3457-61. Date of Electronic Publication: 2011 Apr 03. - Publication Year :
- 2011
-
Abstract
- Novel quaternary ammonium derivatives of N,N-disubstituted (3R)-quinuclidinyl carbamates have been identified as potent M(3) muscarinic antagonists with long duration of action in an in vivo model of bronchoconstriction. These compounds have also presented a high level of metabolic transformation (human liver microsomes). The synthesis, structure-activity relationships and biological evaluation of these compounds are reported.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- Carbamates chemistry
Humans
Inhibitory Concentration 50
Microsomes, Liver metabolism
Molecular Structure
Muscarinic Antagonists chemistry
Quaternary Ammonium Compounds chemical synthesis
Quaternary Ammonium Compounds chemistry
Quaternary Ammonium Compounds pharmacology
Quinuclidines chemical synthesis
Quinuclidines chemistry
Quinuclidines pharmacology
Time Factors
Carbamates chemical synthesis
Carbamates pharmacology
Drug Discovery
Microsomes, Liver drug effects
Muscarinic Antagonists chemical synthesis
Muscarinic Antagonists pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21524581
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.03.096