Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Steven W. Louie"'
Autor:
Hua Gao, Christopher D. Hein, Steven W. Louie, Marian C. Bryan, Xiaoyang Xia, Bernd A. Bruenner, Elizabeth M. Doherty, Heather Eastwood
Publikováno v:
ACS Combinatorial Science. 15:503-511
A platform that incorporates computational library design, parallel solution-phase synthesis, continuous flow hydrogenation, and automated high throughput purification and reformatting technologies was applied to the production of a 120-member librar
Autor:
Samer Chmait, Adrie D. Jones, Amy Porter, Kristin L. Andrews, Xiaoning Zhao, Jennifer R. Allen, Shannon Rumfelt, Wenge Zhong, Essa Hu, James R. Falsey, Robert M. Rzasa, Steven W. Louie, James J. S. Treanor, Ning Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:7371-7375
We report the discovery of a novel series of biaryl ethers as potent and selective PDE10A inhibitors. Structure-activity studies improved the potency and decreased Pgp-mediated efflux found in the initial compound 4. X-ray crystallographic studies re
Autor:
Patrick T. Ronaldson, Laurent Salphati, Björn Bauer, Steven W. Louie, Ayman El-Kattan, Hong Shen
The American Association of Pharmaceutical Scientists/International Transporter Consortium Joint Workshop on Drug Transporters in absorption, distribution, metabolism, and excretion was held with the objective of discussing innovative advances in tra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ad66276e43202458f71cac7ab3d5927
https://europepmc.org/articles/PMC5466066/
https://europepmc.org/articles/PMC5466066/
Autor:
Yuan Cheng, Matthew R. Kaller, Steven W. Louie, Martin Citron, Lewis D. Pennington, Daniel S. La, Matthew Weiss, Stephen J. Wood, Wenge Zhong, Michael Croghan, Toni Williamson, Scott Harried, James Brown, Kui Chen, Tisha San Miguel, Ronke Imbeah-Ampiah, Holger Monenschein, Qiufen Xue, Hongbing Huang, Patricia Lopez, Claire Rattan, Thomas Dineen, Daniel B. Horne, E. Allen Sickmier, Dean Hickman, Safura Babu-Khan, Charles Kreiman, Vivian S. W. Li, Paul H. Wen, Michael D. Bartberger, Russell Graceffa, Robert C. Wahl, Thomas T. Nguyen, Bryant Yang, Ted Judd, Joel Esmay, Vinod F. Patel, Stephen Hitchcock
Publikováno v:
Journal of Medicinal Chemistry. 55:9009-9024
A series of potent hydroxyethyl amine (HEA) derived inhibitors of β-site APP cleaving enzyme (BACE1) was optimized to address suboptimal pharmacokinetics and poor CNS partitioning. This work identified a series of benzodioxolane analogues that posse
Autor:
Paul H. Wen, Robert C. Wahl, Michael Croghan, Ronke Imbeah-Ampiah, Paul Acton, Stephen J. Wood, Charles Kreiman, Vivian S. W. Li, Qiufen Xue, Lewis D. Pennington, Safura Babu-Khan, Daniel B. Horne, Thomas Dineen, Wenge Zhong, Scott Harried, Douglas A. Whittington, Dean Hickman, James Brown, Martin Citron, Matthew Weiss, Daniel S. La, Holger Monenschein, Bryant Yang, E. Allen Sickmier, Tisha San Miguel, Robert T. Dunn, Russell Graceffa, Patricia Lopez, Toni Williamson, Hongbing Huang, Yuan Cheng, Kui Chen, Matthew R. Kaller, Michael D. Bartberger, Steven W. Louie, Hugo M. Vargas, Stephen Hitchcock, Thomas T. Nguyen, Vinod F. Patel, Ted Judd, Joel Esmay
Publikováno v:
Journal of Medicinal Chemistry. 55:9025-9044
We have previously shown that hydroxyethylamines can be potent inhibitors of the BACE1 enzyme and that the generation of BACE1 inhibitors with CYP 3A4 inhibitory activities in this scaffold affords compounds (e.g., 1) with sufficient bioavailability
Autor:
Timothy Powers, Stephen J. Wood, Ted Judd, Vivian S. W. Li, James Brown, E. Allen Sickmier, Klaus Michelsen, David J. St. Jean, Yi Luo, Dean Hickman, Yuan Cheng, Kui Chen, Stephen Hitchcock, Steven W. Louie, Patricia Lopez, Brad Jordan, Thomas Nixey, Robert T. Fremeau, Michael D. Bartberger, Paul H. Wen, Robert C. Wahl, Claire Rattan
Publikováno v:
Journal of Medicinal Chemistry. 54:5836-5857
Using fragment-based screening of a focused fragment library, 2-aminoquinoline 1 was identified as an initial hit for BACE1. Further SAR development was supported by X-ray structures of BACE1 cocrystallized with various ligands and molecular modeling
Autor:
Sarah Walter, Roger Pham, Savannah J Kerr, Joel D Esmay, Xiaochun Zhu, Michael E. Fitzsimmons, Raju Subramanian, Gary L Skiles, Marcus Soto, Steven W Louie, Sarah F Wilson, Katheryne Z Edson, Mylo Wagner
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 44(8)
AMG 416 (etelcalcetide) is a novel synthetic peptide agonist of the calcium-sensing receptor composed of a linear chain of seven d-amino acids (referred to as the d-amino acid backbone) with a d-cysteine linked to an l-cysteine via a disulfide bond.
Autor:
Jerome H. Hochman, Edward J. Carlini, Roy Eisenhandler, Bing Li, Qin Mei, Masayo Yamazaki, Brenda F. Leake, Steven W. Louie, Catherine Booth-Genthe, Thomas H. Rushmore, Richard B. Kim
Publikováno v:
Journal of Pharmacological and Toxicological Methods. 54:78-89
Introduction P-glycoprotein is localized in numerous tissues throughout the body and plays an important role in the disposition of many xenobiotics. The contribution of P-glycoprotein-mediated drug transport is being evaluated in early drug discovery
Autor:
Oleg Epstein, Stephen J. Wood, Dean Hickman, Paul H. Wen, Robert C. Wahl, Thomas Dineen, Robert T. Fremeau, Alan C. Cheng, Russell Graceffa, Y.-H. Kiang, Steven W. Louie, Hongbing Huang, Kui Chen, Vinod F. Patel, Douglas A. Whittington, Yi Luo, Daniel S. La
Publikováno v:
Journal of medicinal chemistry. 55(21)
A structure- and property-based drug design approach was employed to identify aminooxazoline xanthenes as potent and selective human β-secretase inhibitors. These compounds exhibited good isolated enzyme, cell potency, and selectivity against the st
Autor:
Yi Luo, Matthew Weiss, Stephen J. Wood, Tom Dineen, Kui Chen, Jodi Bradley, Hongbing Huang, Ted Judd, Patricia Lopez, Li Zhu, Yuan Cheng, Patricia Amarante, Dean Hickman, Bryant Yang, Paul Acton, Safura Babu-Khan, Steven W. Louie, Mathew Kaller, Joel Esmay, Jan Zhang, Russell Graceffa, Wenge Zhong, Daniel B. Horne, Toni Williamson, Paul H. Wen, Robert C. Wahl
Publikováno v:
Alzheimer's & Dementia. 8