Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Linda L. Coughenour"'
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:489-493
As part of an on-going effort to investigate the chemical space requirements for D(2)/5-HT(2A) receptor antagonists as atypical antipsychotics, new 1-aminoindanes were synthesized. The replacement of the heterocycle (oxindole) in ziprasidone with a c
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4560-4563
Several new, potent dopamine subtype 2 (DA D2) active compounds with serotonin subtype 2A (5-HT2A) pharmacology are presented. 8-Substituted 3,4-dihydroquinolinones, tetrahydroquinolines, and N-acyl tetrahydroquinolines were evaluated in primary assa
Autor:
Edward R. Whittemore, Minhtam Tran, David Rock, Richard M. Woodward, Zhang-Lin Zhou, Sui Xiong Cai, Christopher S. Konkoy, Stephen A. Espitia, Lawrence D. Wise, Christopher F. Bigge, John F. W. Keana, Jon E. Hawkinson, Eckard Weber, Peter A. Boxer, Linda L. Coughenour
Publikováno v:
Journal of Medicinal Chemistry. 42:2993-3000
A structure-based search and screen of our compound library identified N-(2-phenoxyethyl)-4-benzylpiperidine (8) as a novel N-methyl-D-aspartate (NMDA) receptor antagonist that has high selectivity for the NR1/2B subunit combination (IC(50) = 0.63 mi
Autor:
Albert W. Probert, Peter A. Boxer, SA Borosky, Kevin K.W. Wang, Linda L. Coughenour, Iradj Hajimohammadreza, Frank W. Marcoux
Publikováno v:
The Journal of Neuroscience. 15:4093-4101
Calcium/calmodulin-dependent protein kinase-II (CamK-II) is a major neuronal protein which plays a significant role in the cellular process of long-term potentiation (LTP), and vesicular release of neurotransmitters. Here, we show that KN-62, 1-[N,O-
Autor:
Thomas Charles Malone, Gregory W. Campbell, Elsebet Ø. Nielsen, Peter A. Boxer, Jorgen Drejer, Christopher F. Bigge, Frank Wätjen, Frank W. Marcoux, David M. Rock, Leif Helth Jensen, Leonard Joseph Lescosky, Linda L. Coughenour
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:371-376
Autor:
Walter H. Moos, Stephen Joseph Johnson, Sharie L. Myers, Michael R. Pavia, Suzanne R. Kesten, Roy D. Schwarz, Robert E. Davis, Sheila H. Hobbs, Linda L. Coughenour, David T. Dudley
Publikováno v:
ChemInform. 22
Autor:
Leonard Joseph Lescosky, Peter A. Boxer, Christopher F. Bigge, E. Oe. Nielen, Thomas Charles Malone, David M. Rock, Gregory W. Campbell, Frank W. Marcoux, F. Waetjen, L. H. Jensen, J. Drejer, Linda L. Coughenour
Publikováno v:
ChemInform. 25
Autor:
Susan Fisher, Anthony Jerome Thomas, Sharie L. Myers, Michael R. Pavia, Walter H. Moos, Kathryn B. Sanders, Robert E. Davis, Linda L. Coughenour
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 2:803-808
There is considerable interest in muscarinic acetylcholine receptor (mAChR) subtype selective agents as cholinomimetics for the treatment of senile dementia of the Alzheimer's type (SDAT). A series of substituted analogs similar to the muscarinic ago
Autor:
Laura J. Brahce, Daniel F. Ortwine, Christopher F. Bigge, Daniel Martin Retz, Linda L. Coughenour, Frank W. Marcoux, Graham Johnson, Albert W. Probert, James T. Drummond
Publikováno v:
Journal of Medicinal Chemistry. 35:1371-1384
A series of N-substituted alpha-amino acids containing terminal phosphonic acid groups has been synthesized as potential N-methyl-D-aspartate (NMDA) receptor antagonists. NMDA receptor affinity was determined by displacement of a known ligand ([3H]CP
Autor:
Linda L. Coughenour, Christopher F. Bigge, Cynthia M. Hanchin, James T. Drummond, Jiang-Ping Wu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 2:207-212
6-Phosphonoalkyltetrahydro-4-pyrimidinecarboxylic acids and their acyclic equivalents were determined to be competitive N-methyl-D-aspartic acid (NMDA) receptor antagonists using a [3H]-CPP binding assay. Results suggest that internal hydrogen bondin