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Your search keyword '"Nozulak, Joachim"' showing total 3 results
Start Over Author "Nozulak, Joachim" Publisher elsevier science ltd
3 results on '"Nozulak, Joachim"'

1. 6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.

Author

Orain D, Ofner S, Koller M, Carcache DA, Froestl W, Allgeier H, Rasetti V, Nozulak J, Mattes H, Soldermann N, Floersheim P, Desrayaud S, Kallen J, Lingenhoehl K, and Urwyler S

Subjects
Administration, Oral, Animals, Anticonvulsants administration & dosage, Anticonvulsants chemistry, Crystallography, X-Ray, Disease Models, Animal, Dose-Response Relationship, Drug, Mice, Mice, Inbred DBA, Models, Molecular, Molecular Structure, Quinazolinones administration & dosage, Quinazolinones chemistry, Seizures drug therapy, Stereoisomerism, Structure-Activity Relationship, Sulfonamides administration & dosage, Sulfonamides chemistry, Anticonvulsants pharmacology, Quinazolinones pharmacology, Receptors, AMPA antagonists & inhibitors, Sulfonamides pharmacology
Abstract

A new set of quinazolinedione sulfonamide derivatives as competitive AMPA receptor antagonist with improved properties compared to 1 is disclosed. By modulating physico-chemical properties, compound 29 was identified with a low ED(50) of 5.5mg/kg in an animal model of anticonvulsant activity after oral dosage., (Copyright © 2011. Published by Elsevier Ltd.)

Published
2012
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2. Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor.

Author

Hintermann S, Hurth K, Nozulak J, Tintelnot-Blomley M, Aichholz R, Blanz J, Kaupmann K, and Mosbacher J

Subjects
Benzodiazepines metabolism, Binding Sites, Drug Stability, GABA-A Receptor Agonists chemistry, GABA-A Receptor Agonists pharmacology, Inhibitory Concentration 50, Ligands, Molecular Structure, Pyrazoles metabolism, Structure-Activity Relationship, Benzodiazepines chemistry, GABA-A Receptor Agonists chemical synthesis, Pyrazoles chemistry, Receptors, GABA-A metabolism
Abstract

A novel series of agonists at the benzodiazepine binding site of the GABA(A) receptor was prepared by functionalizing a known template. Adding substituents to the pyrazolone-oxygen of CGS-9896 led to a number of compounds with selectivities for either α2- or α1-containing GABA(A) receptor subtypes offering an entry into indications such as anxiety and insomnia. In this communication, structure-activity relationship and efforts to increase in vitro stabilities are discussed., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Published
2011
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3. Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.

Author

Enz A, Feuerbach D, Frederiksen MU, Gentsch C, Hurth K, Müller W, Nozulak J, and Roy BL

Subjects
Animals, Binding Sites, Brain metabolism, Humans, Mice, Nicotinic Agonists chemistry, Protein Binding, Rabbits, Receptors, Nicotinic chemistry, alpha7 Nicotinic Acetylcholine Receptor, Lactams chemistry, Nicotinic Agonists metabolism, Receptors, Nicotinic metabolism
Abstract

A novel class of alpha7 nicotinic acetylcholine receptor (nAChR) agonists has been discovered through high-throughput screening. The cis gamma-lactam scaffold has been optimized to reveal highly potent and selective alpha7 nAChR agonists with in vitro activity and selectivity and with good brain penetration in mice.

Published
2009
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