Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Lana Louise Smith-Keenan"'
Autor:
Steven J. Taylor, Asitha Abeywardane, Shuang Liang, Zhaoming Xiong, John R. Proudfoot, Bennett Sandy Farmer, Donghong A. Gao, Alexander Heim-Riether, Lana Louise Smith-Keenan, Ingo Muegge, Yang Yu, Qiang Zhang, Donald Souza, Mark Panzenbeck, Daniel Goldberg, Melissa Hill-Drzewi, Mariana Margarit, Brandon Collins, John Xiang Li, Ljiljana Zuvela-Jelaska, Jun Li, Neil A. Farrow
Publikováno v:
ACS Omega, Vol 6, Iss 29, Pp 18635-18650 (2021)
Externí odkaz:
https://doaj.org/article/28925716e0524cb7af79c7a4126b692b
Autor:
John Xiang Li, Steven John Taylor, Mariana Margarit, Jun Li, Yu Yang, Qiang Zhang, Ingo Muegge, Melissa Hill-Drzewi, Alexander Heim-Riether, Mark Panzenbeck, Asitha Abeywardane, Zhaoming Xiong, Daniel R. Goldberg, Bennett Sandy Farmer, Gao Donghong A, Ljiljana Zuvela-Jelaska, John R. Proudfoot, Shuang Liang, Donald Souza, Lana Louise Smith-Keenan, Neil A. Farrow, Brandon Collins
Publikováno v:
ACS Omega
ACS Omega, Vol 6, Iss 29, Pp 18635-18650 (2021)
ACS Omega, Vol 6, Iss 29, Pp 18635-18650 (2021)
Here, we described the design, by fragment merging and multiparameter optimization, of selective MMP-13 inhibitors that display an appropriate balance of potency and physicochemical properties to qualify as tool compounds suitable for in vivo testing
Autor:
E. Michael August, Lana Louise Smith Keenan, Jun Li, S. Mariana Margarit, Alexander Heim-Riether, Hans-Dieter Junker, Kathleen Haverty, Neil A. Farrow, Brandon Collins, Bennett T. Farmer, Thomas Neumann, Shuang Liang, John R. Proudfoot, Renate Sekul, Qiang Zhang, Donghong Amy Gao, Steven John Taylor, Zhaoming Xiong, Neil Moss, Melissa Hill-Drzewi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5321-5324
Discovery and optimization of potency and selectivity of a non-Zn-chelating MMP-13 inhibitor with the aid of protein co-crystal structural information is reported. This inhibitor was observed to have a binding mode distinct from previously published
Publikováno v:
Organic Process Research & Development. 11:60-63
A new procedure for the practical synthesis of (S)-2-(cyclopentyloxycarbonyl)amino-8-nonenoic acid, a key building block for BILN 2061, an HCV NS3 protease inhibitor, has been developed. The key step features a kinetic resolution of racemic 2-acetyla
Autor:
Lana Louise Smith-Keenan, Paul Kreye, Wendelin Samstag, Thomas Nicola, Victor Fuchs, XuWu Feng, Jinghua Xu, Jana Vitous, Earl Spinelli, Rogelio P. Frutos, Jonathan Tan, Eric Winter, Robert D. Simpson, Li Zhang, Fabrice Gallou, Michael D. Ridges, Nathan K. Yee, Vittorio Farina, Marvin Johnson, Xiao-Jun Wang, Nizar Haddad, Ioannis N. Houpis, Xudong Wei, Michael Brenner, Kai Donsbach, Yibo Xu
Publikováno v:
The Journal of Organic Chemistry. 71:7133-7145
A multistep scalable synthesis of the clinically important hepatitis C virus (HCV) protease inhibitor BILN 2061 (1) is described. The synthesis is highly convergent and consists of two amide bond formations, one etherification, and one ring-closing m
Autor:
Bruno Haché, Vittorio Farina, Marvin Johnson, Pierre L. Beaulieu, Christian Brochu, Lana Louise Smith-Keenan, Nathan K. Yee, Jean-Simon Duceppe, Rogelio P. Frutos, Victor Fuchs, Anne-Marie Faucher, Nizar Haddad, Ioannis N. Houpis
Publikováno v:
Synthesis. 2006:2563-2567
Herein we describe the development of an efficient, safe and practical process for the synthesis of 7-methoxy-2-(2-amino-4-thiazolyl)quinoline. Our new process allowed for a more convergent approach and eliminates the use of potentially dangerous rea
Autor:
Shuang Liang, Kathleen Haverty, Donghong Amy Gao, Jun Li, Xiang Li, Sabine Schlyer, Alexander Heim-Riether, Melissa Hill-Drzewi, Steven John Taylor, Steluta Mariana Margarit, Lana Louise Smith Keenan, Neil Moss, Nelamangala V. Nagaraja, Xianhua Cao, Dieter Wiedenmayer, Neil A. Farrow, Kyle E. Harrington, Brandon Collins, E. Michael August, Leonard Ciccarelli, Rene Roman, Bernd Wellenzohn, Zhaoming Xiong, Laura Amodeo, John R. Proudfoot
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(17)
SAR studies to improve the selectivity and metabolic stability of a class of recently discovered MMP-13 inhibitors are reported. Improved selectivity was achieved by modifying interactions with the S1' pocket. Metabolic stability was improved through
Autor:
Neil Moss, Yu Yang, Asitha Abeywardane, Gary O. Caviness, Wang Mao, Ernest L. Raymond, Jennifer A. Kowalski, Jiang-Ping Wu, Amy Gao, Elliott Klein, Derek Cogan, Debra Jeanfavre, Younggi Choi, Lana Louise Smith-Keenan, Donna Skow, Roger J. Snow, Frank Wu, Daniel R. Goldberg, Alexander Heim-Riether, Philip D. Ramsden, Miller Craig Andrew
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. (21):5277-5283
Compound 1 ((4-amino-3,5-dichlorophenyl)-1-(4-methylpiperidin-1-yl)-4-(2-nitroimidazol-1-yl)-1-oxobutane-2-sulfonamido) was discovered to be a 690nM antagonist of human CCR10 Ca2+ flux. Optimization delivered (2R)-4-(2-cyanopyrrol-1-yl)-S-(1H-indol-4