Zobrazeno 1 - 10
of 12
pro vyhledávání: '"J. H. Krushinski"'
Autor:
Clint Duane Walker, James E. Audia, John Mehnert Schaus, Nika Adham, John M. Zgombick, J. H. Krushinski, Daniel Timothy Kohlman, Sidney Xi Liang, Yao-Chang Xu
Publikováno v:
Journal of Medicinal Chemistry. 42:526-531
It has been observed that reported 5-HT1D receptor agonists have at least one heteroatom (N, O, or S) on the 5-substituent of the indole. This has led to the hypothesis that a 5-substituent capable of participating in hydrogen bonding is critical for
Autor:
Bruce D. Gitter, Steven S. Y. Cho, Diane C. Waters, Donald R. Gehlert, Thomas Alan Crowell, Brian Stephen Muehl, Penny G. Threlkeld, Kirk W. Johnson, J. H. Krushinski, Karen Lynn Lobb, Robert F. Bruns, Philip Arthur Hipskind, Domenico Regoli, Lee A. Phebus, Nixon James Arthur, Smriti Iyengar, J. Jeffry Howbert, Dominic L. Li, Foreman Mark Mortensen, Norman R. Mason, Rosa Maria A. Simmons
Publikováno v:
ChemInform. 27
Early structure−activity studies on racemic tryptophan ester and amide NK-1 antagonists 5−7 led to the discovery that the potency of the series could be markedly increased by moving the carbonyl function in these molecules to an off-chain positio
ChemInform Abstract: N-Methyl-5-tert-butyltryptamine: A Novel, Highly Potent 5-HT1D Receptor Agonist
Autor:
Sidney Xi Liang, Yao-Chang Xu, Daniel Timothy Kohlman, John M. Zgombick, Nika Adham, J. H. Krushinski, Clint Duane Walker, John Mehnert Schaus, James E. Audia
Publikováno v:
ChemInform. 30
It has been observed that reported 5-HT1D receptor agonists have at least one heteroatom (N, O, or S) on the 5-substituent of the indole. This has led to the hypothesis that a 5-substituent capable of participating in hydrogen bonding is critical for
Autor:
Dennis Charles Thompson, Frank P. Bymaster, Louise Wallace, E. E. Beedle, David W. Robertson, Peter Thaddeus Gallagher, Stephen N. Mitchell, J. H. Krushinski, David T. Wong, Jeremy Findlay
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(24)
A series of naphthalenyloxy-arylpropylamines have been prepared and are demonstrated to be inhibitors of both serotonin and norepinephrine reuptake. One member of this series, duloxetine (Cymbalta) has proven to be effective in clinical trials for th
Autor:
Steven S. Y. Cho, Penny G. Threlkeld, Nixon James Arthur, Robert F. Bruns, Lee A. Phebus, Thomas Alan Crowell, Karen Lynn Lobb, Kirk W. Johnson, Donald R. Gehlert, Diane C. Waters, Bruce D. Gitter, Brian Stephen Muehl, J. H. Krushinski, Norman R. Mason, Rosa Maria A. Simmons, Domenico Regoli, J. Jeffry Howbert, Dominic L. Li, Foreman Mark Mortensen, Smriti Iyengar, Philip Arthur Hipskind
Publikováno v:
Journal of medicinal chemistry. 39(3)
Early structure-activity studies on racemic tryptophan ester and amide NK-1 antagonists 5-7 led to the discovery that the potency of the series could be markedly increased by moving the carbonyl function in these molecules to an off-chain position as
Publikováno v:
Clinical Neuropharmacology. 15:439B
Autor:
J. H. Krushinski, R. C. Rathbun, David T. Wong, J D Leander, David W. Robertson, E. E. Beedle
Publikováno v:
Journal of Medicinal Chemistry. 29:1577-1586
A recently discovered and structurally distinct class of antiepileptic drugs is the (arylalkyl)imidazoles. Two independently discovered representatives of this class, denzimol (alpha-[4-(2-phenylethyl)phenyl]-1H-imidazole-1-ethanol) and nafimidone (2
Autor:
David W. Robertson, H. Wilson, E. E. Beedle, Hayes Js, G. D. Pollock, J. H. Krushinski, V. L. Wyss
Publikováno v:
Journal of medicinal chemistry. 28(6)
Recently several noncatecholamine, nonglycoside cardiotonic drugs have been discovered that possess both inotropic and vasodilator activities in experimental animals and man. Prototypical compounds include amrinone, sulmazole, and fenoximone. We inve
Publikováno v:
ChemInform. 18
In the 1,3-dihydro-5-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)-2H-indol-2-one series of cardiotonics, we found that a spirocycloalkyl ring may be annealed to the 3-position of the indolone moiety while retaining inotropic activity. An inverse relation
Publikováno v:
Journal of medicinal chemistry. 30(4)
The cardiotonic 1,3-dihydro-3,3-dimethyl-5-(1,4,5,6-tetrahydro-6-oxo-3- pyridazinyl)-2H-indol-2-one (1, LY195115) is a potent, competitive inhibitor (Ki = 80 nM) of sarcoplasmic reticulum derived phosphodiesterase (SR-PDE). Moreover, the compound is