Zobrazeno 1 - 10
of 25
pro vyhledávání: '"David L. Saussy"'
Autor:
Bryan W. Sherman, Jason D. Speake, M. Jeffrey Gobel, Deanna T. Garrison, Eric C. Bigham, Frank Navas, Paul E. Irving, David L. Saussy, James A Liacos, Michael J. Bishop, Stephen J. Hodson
Publikováno v:
Journal of Medicinal Chemistry. 45:2229-2239
A series of 2'-alkylthio-2-(anilinomethyl)imidazolines were prepared to examine the effect of the alkyl group size, sulfur oxidation state, and phenyl ring substitution on ligand binding and agonism of alpha-adrenergic receptor subtypes alpha1a, alph
Publikováno v:
Journal of Pharmacological and Toxicological Methods. 42:237-244
Binding assays have long been used to determine compound affinity and selectivity for various seven-transmembrane receptors. Over time, the degree of complexity has significantly reduced, whereas the throughput of the various assays has greatly incre
Autor:
David L. Saussy, J. Alan Menius, Tony D. Choi, Michael W. Lutz, Aaron S. Goetz, Paul L. Domanico, Rebecca Gooding Laskody
Publikováno v:
Drug Discovery Today. 1:277-286
Novel methods in molecular biology and advanced technologies have given pharmaceutical research laboratories the capability to test combinatorial libraries rapidly against large numbers of potential targets. Methods to identify optimal assay conditio
Publikováno v:
Biochemistry. 35:14312-14317
The alpha 1-adrenergic receptors (alpha 1-AR) belong to the G-protein coupled seven-transmembrane biogenic amine receptor family. Three subtypes have been successfully cloned in the alpha 1-adrenergic receptor family, and they share 50% identical ami
Autor:
Elisabeth A. Schmittling, William T. Jackson, J. Scott Sawyer, David L. Saussy, S. Richard Baker, Philip Marder, Bach Nicholas J, Larry L. Froelich
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:2077-2082
We report the preparation and pharmacologic activity of three spatial analogues of LY292728, a highly potent xanthone dicarboxylic LTB4 receptor antagonist. Molecular modeling of these compounds has helped to further elucidate the nature of the secon
Autor:
Nancy Bowling, William L. Kurtz, Gerald W. Dorn, Kellie A. Brune, Gregory P. Dubé, David L. Saussy, Dale E. Mais
Publikováno v:
Journal of Molecular and Cellular Cardiology. 26:915-923
Thromboxane A2 (TXA2) and prostaglandin H2 (PGH2) induce platelet aggregation and are potent vasoconstrictors, and they have been implicated in coronary vasospasm and myocardial infarction. The TXA2 mimetic [1S-(1α, 2β (5Z), 3α (1E, 3S*), 4α)]-7-
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:795-800
QSAR models for a series of o-phenylphenol LTB 4 receptor antagonist have been developed with regression analysis. These models related specific features, electronic, size and shape, of the substituent with biological activity. The models have predic
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:1985-1990
The preparation and activity of a series of hydroxyacetophenone/diaryl ether LTB 4 receptor antagonists are described. The key acid-substituted diaryl ether moiety is discussed in relation to the spatial and functional group requirements of the LTB 4
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:1981-1984
The preparation and pharmacologic activity of two new hybrid LTB4 receptor antagonists, 1 and 2 (LY282210), are reported. These compounds are among the most potent in vitro LTB4 receptor antagonists yet described, and add new insight into the critica
Autor:
Larry L. Froelich, Carlos R. Roman, Sandra L. Cockerham, Floreancig Paul Edward, William T. Jackson, Philip Marder, Michael J. Sofia, Peter W. Stengel, Steven A. Silbaugh, Jerome H. Fleisch, David L. Saussy
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:1147-1152
7-[4-Acetyl-2-ethyl-5-hydroxyphenoxy)propoxy]-3,4-dihydro-8-propyl-2H-1-benzopyran-2-carboxylic acid sodium salt 7 (LY247826) and several 7-[3-(4-acetyl-2-ethyl-5-hydroxyphenoxy)propoxy)-2-propylphenoxy] acetic acid analogues were prepared as LTB4 re