Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Paul R. Fatheree"'
Autor:
Whitney Krey-Epstein, Elad Kaufman, Erik Sandvik, Susan L. Calhoun, Paul R. Fatheree, Melanie A. Kleinschek, Joe Budman, Emma Gordon, Reuben Sana
Publikováno v:
Airway pharmacology and treatment.
Clinical studies with biologics have demonstrated the importance of cytokines in the pathobiology of asthma. However, redundancy and heterogeneity in the asthma cytokine networks may limit the efficacy of single cytokine-targeting biologics. Thus, we
Autor:
Craig M. Hill, Donavon McConn, Laxminarayan G Hegde, Roland Gendron, Brooke Blair, Keith Jendza, Joe Budman, Paul R. Fatheree, Daniel Marquess, R. Murray McKinnell, Cecile Yu, Sharath S. Hegde, Seok-Ki Choi, Uwe Klein
[Image: see text] Dual inhibition of angiotensin-converting enzyme (ACE) and neprilysin (NEP) by drugs such as omapatrilat produces superior antihypertensive efficacy relative to ACE inhibitors but is associated with a higher risk of life-threatening
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d8ec5793446e9f5c0388334fd310b518
https://europepmc.org/articles/PMC6331171/
https://europepmc.org/articles/PMC6331171/
Autor:
Jeng-Pyng Shaw, Daniel Marquess, R. Murray McKinnell, Paul R. Fatheree, David Beattie, Scott R. Armstrong, Daniel D. Long, Ross G. Vickery
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4210-4215
The discovery of a series of 5-HT4 receptor agonists based on a novel 2-alkylbenzimidazole aromatic core is described. Optimization of the 2-substituent of the benzimidazole ring led to a series of agonists with subnanomolar binding affinity and mode
Autor:
Roopa Rai, Kyle Elrod, William D. Shrader, James W. Janc, Yong Li, Lynne Cregar, Wendy B. Young, Aleksandr Kolesnikov, Thomas E. Jenkins, Paul R. Fatheree, Brad A. Katz, Erik Verner, Paul A. Sprengeler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:710-713
Inhibition of coagulation proteases such as thrombin, fXa, and fVIIa has been a focus of ongoing research to produce safe and effective antithrombotic agents. Herein, we describe a unique zinc-mediated chelation strategy to streamline the discovery o
Autor:
Kevin M. Krause, Bettina Bazzini, J. Kevin Judice, Burton G. Christensen, Michael R. Leadbetter, Dane E. Karr, Sean G. Trapp, Elizabeth Soriano, Jeng-Pyng Shaw, Paul R. Fatheree, Kelly L. Quast, Lam Bernice M T, Martin S. Linsell, Matthew B. Nodwell, Terry X. Wu, John L. Pace, Jenny D. Villena, Stacy M. Adams
Publikováno v:
The Journal of Antibiotics. 57:326-336
Novel derivatives of N-decylaminoethylvancomycin (2), containing appended hydrophilic groups were synthesized and their antibacterial activity and ADME properties were evaluated. The compounds were prepared by reacting amines with the C-terminus (C-)
Autor:
Paul R. Fatheree, Jacqueline A.M. Smith, Patrick P. Humphrey, David Beattie, S. Derek Turner, Seok-Ki Choi, Roland Gendron, Daniel Marquess, Goldblum Adam A, Ross G. Vickery, Jeng Pyng Shaw, Scott R. Armstrong, Daniel D. Long, Lan Jiang, Daniel Genov
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(19)
Utilization of Theravance’s multivalent approach to drug discovery towards 5-HT 4 receptor agonists with a focus on identification of neutral (non-charged at physiological pH) secondary binding groups is described. Optimization of a quinolone-tropa
Autor:
David Beattie, Daniel D. Long, S. Derek Turner, Paul R. Fatheree, Jacqueline A.M. Smith, Scott R. Armstrong, Seok-Ki Choi, Roland Gendron, Jeng Pyng Shaw, Goldblum Adam A, Daniel Marquess, Ross G. Vickery, Patrick P. Humphrey
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(14)
Further application of our multivalent approach to drug discovery directed to 5-HT4 receptor agonists is described. Optimization of the linker and secondary binding amine in the indazole-tropane primary binding group series, for binding affinity and
Autor:
Scott R. Armstrong, Seok-Ki Choi, Jeng-Pyng Shaw, David Beattie, Goldblum Adam A, S. Derek Turner, Daniel D. Long, R. Murray McKinnell, Ross G. Vickery, Daniel Marquess, Paul R. Fatheree, Jacqueline A.M. Smith, Roland Gendron, Patrick P. Humphrey
Publikováno v:
Journal of medicinal chemistry. 52(17)
5-HT(4) receptor agonists such as tegaserod have demonstrated efficacy in the treatment of constipation predominant irritable bowel syndrome (IBS-C), a highly prevalent disorder characterized by chronic constipation and impairment of intestinal propu
Autor:
Sharath S. Hegde, Matthew B. Nodwell, Martin S. Linsell, Kevin M. Krause, Paul R. Fatheree, Daniel Marquess, David W. Green, John L. Pace, James B. Aggen, Koné Kaniga, Sean G. Trapp, Jason P. Chinn, Seok-Ki Choi, J. Kevin Judice, Burton G. Christensen, Michael R. Leadbetter, S. Derek Turner, Daniel D. Long, Edmund J. Moran
Publikováno v:
The Journal of antibiotics. 61(10)
Further investigations towards novel glycopeptide/beta-lactam heterodimers are reported. Employing a multivalent approach to drug discovery, vancomycin and cephalosporin synthons, 4, 2, 5 and 10, 18, 25 respectively, were chemically linked to yield h
Autor:
R. Murray McKinnell, Scott R. Armstrong, David T. Beattie, Seok-Ki Choi, Paul R. Fatheree, Roland A. L. Gendron, Adam Goldblum, Patrick P. Humphrey, Daniel D. Long, Daniel G. Marquess, J. P. Shaw, Jacqueline A. M. Smith, S. Derek Turner, Ross G. Vickery
Publikováno v:
Journal of Medicinal Chemistry; Sep2009, Vol. 52 Issue 17, p5330-5343, 14p