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Aryl Amides (aryl + amide)
Selected AbstractsChemInform Abstract: Flexible Palladium-Catalyzed Amidation Reactions for the Synthesis of Complex Aryl Amides.CHEMINFORM, Issue 35 2010Alan Hennessy No abstract is available for this article. [source] A Novel Approach for the Synthesis of Aryl Amides.CHEMINFORM, Issue 50 2007Ahmad Shaabani Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Preparation of novel azabicyclic amines and ,7 nicotinic acetylcholine receptor activity of derived aryl amidesJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 1 2008Daniel P. Walker Three new azabicyclic amines, namely exo -3-amino-1-azabicyclo[3.2.1]octane, 3-amino-1-azabicyclo-[3.2.2]nonane and exo -6-amino-8-azabicyclo[3.2.1]octane, have been designed and prepared as isosteres of 3-aminoquinuclidine. Aryl amides derived from each series were prepared and tested in an ,7 nicotinic acetylcholine receptor assay as part of a drug discovery program to treat the cognitive deficits in schizophrenia. All new amides showed significant ,7 nAChR activity and one series displayed potent ,7 activity equal to the quinuclidine series. [source] Cellular Internalization of Water-Soluble Helical Aromatic Amide FoldamersCHEMBIOCHEM, Issue 12 2010Jone Iriondo-Alberdi Dr. Abstract The intracellular transport of drugs and therapeutics represents one of the most exciting and challenging areas at the interface of chemistry, biology, and medicine. Most of the effort in this field so far has been devoted to the development of peptide-based delivery systems that can translocate therapeutic agents into their intracellular targets. More recently, the use of bioinspired non-natural foldamers has resulted in the successful delivery of cargo molecules, which possess a wide range of sizes and physicochemical properties across the cell membrane. We report herein the synthesis of aromatic amide foldamers and their biological evaluation as cell-penetrating agents. By using a well-established synthetic route, a series of fluorescein-labeled cationic aryl amide conjugates has been constructed, and their cellular uptake into various human cell lines has been analyzed by flow cytometry and fluorescence microscopy. The assays revealed that longer oligomers achieve greater cellular translocation, with octamer Q8 proving to be a remarkable vehicle for all three cell lines. Biological studies have also indicated that these helices are biocompatible, thus showing promise in their application as cell-penetrating agents and as vehicles to deliver biologically active molecules into cells. [source] Preparation of novel azabicyclic amines and ,7 nicotinic acetylcholine receptor activity of derived aryl amidesJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 1 2008Daniel P. Walker Three new azabicyclic amines, namely exo -3-amino-1-azabicyclo[3.2.1]octane, 3-amino-1-azabicyclo-[3.2.2]nonane and exo -6-amino-8-azabicyclo[3.2.1]octane, have been designed and prepared as isosteres of 3-aminoquinuclidine. Aryl amides derived from each series were prepared and tested in an ,7 nicotinic acetylcholine receptor assay as part of a drug discovery program to treat the cognitive deficits in schizophrenia. All new amides showed significant ,7 nAChR activity and one series displayed potent ,7 activity equal to the quinuclidine series. [source] | ||||||||||