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.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
-
Carbamates / chemical synthesis*
-
Carbamates / chemistry
-
Carbamates / pharmacology*
-
Drug Discovery*
-
Humans
-
Inhibitory Concentration 50
-
Microsomes, Liver / drug effects*
-
Microsomes, Liver / metabolism
-
Molecular Structure
-
Muscarinic Antagonists / chemical synthesis*
-
Muscarinic Antagonists / chemistry
-
Muscarinic Antagonists / pharmacology*
-
Quaternary Ammonium Compounds / chemical synthesis
-
Quaternary Ammonium Compounds / chemistry
-
Quaternary Ammonium Compounds / pharmacology
-
Quinuclidines / chemical synthesis
-
Quinuclidines / chemistry
-
Quinuclidines / pharmacology
-
Time Factors
Substances
-
Carbamates
-
Muscarinic Antagonists
-
Quaternary Ammonium Compounds
-
Quinuclidines