Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Dennis Michael Downing"'
Autor:
Melanie Kessler, Eric A. Ertel, John Gatfield, Rick D Gaston, Corinna Grisostomi, Thomas Pfeifer, Lubos Remen, Lloyd Simons, Olivier Bezencon, Johannes Mosbacher, Catherine Roch, Richard Moon, Dennis Michael Downing, Markus Rey
Publikováno v:
Journal of Medicinal Chemistry. 59:8398-8411
A series of dihydropyrazole derivatives was developed as potent, selective, and brain-penetrating T-type calcium channel blockers. An optimized derivative, compound 6c, was advanced to in vivo studies, where it demonstrated efficacy in the WAG/Rij ra
Autor:
Noel A. Powell, Robert Ostroski, Cuiman Cai, Mehran Jalaie, Dennis Michael Downing, Daniel D. Holsworth, Wayne L. Cody, John W. Bryant, J. Michael Ryan, Jeremy J. Edmunds
Publikováno v:
Bioorganic & Medicinal Chemistry. 13:2657-2664
Ketopiperazine 2 was designed from a previously published analog. Compound 2 was shown to be a novel, potent inhibitor of renin that, when administered orally, lowered blood pressure in a hypertensive double transgenic (human renin and angiotensinoge
Autor:
Ruben de Kanter, René Roscher, Rick D Gaston, Benno Schindelholz, John Gatfield, Catherine Roch, Olivier Bezencon, Eric A. Ertel, Johannes Mosbacher, Bruno Capeleto, Luboš Remeň, Davide Pozzi, Lloyd Simons, Thomas Pfeifer, Bibia Heidmann, Isabelle Reymond, Melanie Kessler, Corinna Grisostomi, Dennis Michael Downing, Simon Stamm, Richard Moon, Sylvia Richard, Luca Moccia, Romain Siegrist, Michael Toeroek-Schafroth, Elvire Fournier, Markus Rey
Publikováno v:
CHIMIA, Vol 71, Iss 10 (2017)
We describe the discovery and optimization of new, brain-penetrant T-type calcium channel blockers. We present optimized compounds with excellent efficacy in a rodent model of generalized absence-like epilepsy. Along the fine optimization of a chemic
Autor:
Daniel D. Holsworth, Xue-Min Cheng, Chitase Lee, Wayne L. Cody, John W. Bryant, Samarendra N. Maiti, Cuiman Cai, Mohammad Rahim, Michael J. Ryan, Erli Zhang, Patrick I. McConnell, Tingsheng Li, Jeremy J. Edmunds, Dennis Michael Downing, Erasga Noe Ouano, Aparna Kasani, Michael Stier, Rajendra Subedi, Mehran Jalaie, Noel A. Powell, Eric Hall
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(9)
A systematic investigation of the S 3 sub-pocket activity requirements was conducted. It was observed that linear and sterically small side chain substituents are preferred in the S 3 sub-pocket for optimal renin inhibition. Polar groups in the S 3 -
Autor:
Peter G. Blazecka, Emma C. Clay, Wayne L. Cody, Fred L. Ciske, Noel A. Powell, Jeremy J. Edmunds, Dennis Michael Downing, Daniel D. Holsworth
Publikováno v:
ChemInform. 36
Chiral 1-aryl-6-(hydroxymethyl)-2-ketopiperazines can be prepared via an operationally simple, 6-exo epoxide ring-opening cyclization to form the ketopiperazine C6−N1 bond in high yields and with excellent enantiomeric purity.
Autor:
Jeremy J. Edmunds, Peter G. Blazecka, Fred L. Ciske, Dennis Michael Downing, Noel A. Powell, Emma C. Clay, Daniel D. Holsworth, Wayne L. Cody
Publikováno v:
Organic letters. 6(22)
[reaction: see text] Chiral 1-aryl-6-(hydroxymethyl)-2-ketopiperazines can be prepared via an operationally simple, 6-exo epoxide ring-opening cyclization to form the ketopiperazine C6-N1 bond in high yields and with excellent enantiomeric purity.
Autor:
Roger N. Hayes, M. Rose Feng, Jon L. Wright, Dennis Michael Downing, T. A. Pugsley, Leonard T. Meltzer, Thomas G. Heffner, Lawrence D. Wise, Robert G. MacKenzie
Publikováno v:
Journal of medicinal chemistry. 38(26)
Liquid chromatographic-mass spectrometric (LC-MS) analysis of plasma taken from cynomolgus monkeys dosed orally with (R)-(+)-1,2,3,6-tetrahydro-4-phenyl-1-[(3-phenylcyclohexen-1- yl)methyl]pyridine (1), a dopamine (DA) autoreceptor agonist and potent