Zobrazeno 1 - 10
of 26
pro vyhledávání: '"George W. Holland"'
Autor:
Joseph Grimsby, Robert Francis Kester, Aruna Railkar, Cheryl Spence, Nancy-Ellen Haynes, Kevin Richard Guertin, Paige Erin Mahaney, Lida Qi, John Tengi, Wendy Lea Corbett, Fred Thomas Bizzarro, Mark T. Dvorozniak, George W. Holland, Joseph F. Grippo, Franz M. Matschinsky, Darryl W. Hilliard, Ramakanth Sarabu
Publikováno v:
Journal of Medicinal Chemistry. 53:3618-3625
Glucokinase (GK) is a glucose sensor that couples glucose metabolism to insulin release. The important role of GK in maintaining glucose homeostasis is illustrated in patients with GK mutations. In this publication, identification of the hit molecule
Publikováno v:
Journal of Chemical Information and Modeling. 46:2674-2683
In this work, a genetic algorithm (GA) was applied to build up a set of QSPR (quantitative structure-property relationship) models for human absolute oral bioavailability, plasma protein binding, and urinary excretion using the counts of molecular fr
Publikováno v:
Synthetic Communications. 32:1615-1624
Sitaxsentan sodium (1, TBC11251Na) is an ETA selective endothelin antagonist under clinical development for pulmonary arterial hypertension and congestive heart failure. Second generation compounds, as exemplified by TBC2576 (2) are currently under d
Autor:
Vippra Knowles, George W. Holland, E. Radford Decker, Huong Bui, Li Jian, Tommy A. Brock,†,‡ and, Fiona Stavros, Chengde Wu, Li Wen, Natalie Blok, Richard A. F. Dixon, Karin Keller, Andree R. Bourgoyne
Publikováno v:
Journal of Medicinal Chemistry. 44:1211-1216
Sitaxsentan (3, TBC11251) (Wu et al. J. Med. Chem. 1997, 40, 1690) is an orally active ET(A) selective endothelin antagonist that attenuates pulmonary vascular hypertension and cardiac hypertrophy in rats (Tilton et al. Pulm. Pharmacol. Ther. 2000, 1
Autor:
Huong Bui, R J Biediger, George W. Holland, Andree R. Bourgoyne, Natalie Blok, Raju Bore Gowda, Chen Q, Chengde Wu, R. V. Market, Richard A. F. Dixon, Tommy A. Brock, Knowles, Timothy P. Kogan, B. Dupre, Lin S, Decker Er
Publikováno v:
Journal of Medicinal Chemistry. 42:4485-4499
We have previously disclosed the discovery of 2,4-disubstituted anilinothiophenesulfonamides with potent ET(A)-selective endothelin receptor antagonism and the subsequent identification of sitaxsentan (TBC11251, 1) as a clinical development compound
Publikováno v:
ChemInform. 33
Publikováno v:
ChemInform. 33
A solution-phase parallel synthesis of o-phenylenediamines is described. These intermediates were then subsequently converted to benzimidazole scaffolds (three-point diversity) in excellent purities and yields. High-throughput purification of this mu
Publikováno v:
Journal of chemical information and modeling. 47(4)
In this work, two reliable aqueous solubility models, ASMS (aqueous solubility based on molecular surface) and ASMS-LOGP (aqueous solubility based on molecular surface using ClogP as a descriptor), were constructed by using atom type classified solve
Autor:
Vippra Knowles, Huong Bui, George W. Holland, Tony J. You, Junmei Wang, Chengde Wu, Andree R. Bourgoyne, Richard A. F. Dixon, Natalie Blok, E. Radford Decker, Tommy A. Brock, Kurt L. Berens
Publikováno v:
Journal of medicinal chemistry. 47(8)
Sitaxsentan (1) (Wu et al. J. Med. Chem. 1997, 40, 1690) is our first endothelin antagonist being evaluated in clinical trials. It has demonstrated biological effects in an acute hemodynamic study in CHF (Givertz et al. Circulation 2000, 101, 2922),
Autor:
George W. Holland, Kurt L. Berens, Richard A. F. Dixon, Biediger Ronald J, Peter Vanderslice, Darren G. Woodside
Publikováno v:
Pulmonary pharmacologytherapeutics. 17(1)
Airway inflammation is a hallmark of respiratory diseases such as asthma and chronic obstructive pulmonary disease. Cell adhesion molecules play critical roles in the recruitment and migration of cells to sites of inflammation. Not surprisingly, thes