Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Andrea Mcclure"'
Autor:
Kathy Sarris, Philip J. Hajduk, Ihle David C, Diana L. Donnelly-Roberts, Arthur Gomtsyan, Christian Goess, David B. Duignan, Danying Song, Chaohong Sun, Andrea Mcclure, Adrian D. Hobson, Robert H. Stoffel, Anil Vasudevan, John A. Mankovich, Sanjay C. Panchal, A. Chris Krueger, Steven L. Swann, Kenneth M. Comess, Andrew M. Petros, Wilson Noel S, Jill M. Wetter, Paul G. Richardson, Kenton L. Longenecker, Paul M. Jung, Vincent S. Stoll, Amanda W. Dombrowski, Suzanne Mathieu, Justin D. Dietrich, Philip B. Cox
Publikováno v:
Journal of Medicinal Chemistry. 64:417-429
Tumor necrosis factor α (TNFα) is a soluble cytokine that is directly involved in systemic inflammation through the regulation of the intracellular NF-κB and MAPK signaling pathways. The development of biologic drugs that inhibit TNFα has led to
Autor:
Nicholas A. Meanwell, Kevin J. Robbins, Carolyn Diane Dzierba, Rick L. Pieschl, Ramkumar Rajamani, James Herrington, Lorin A. Thompson, Andrea McClure, Yong-Jin Wu, Michele Matchett, Ronald J. Knox, Brian Lee Venables, Jason M. Guernon, Linda J. Bristow, Richard E. Olson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:958-962
Replacement of the piperidine ring in the lead benzenesulfonamide Nav1.7 inhibitor 1 with a weakly basic morpholine core resulted in a significant reduction in Nav1.7 inhibitory activity, but the activity was restored by shortening the linkage from m
Autor:
Kathleen W. Mosure, Michele Matchett, Ronald J. Knox, Richard E. Olson, Joanne J. Bronson, Nicholas A. Meanwell, Matthew G. Soars, Linda J. Bristow, Ramkumar Rajamani, James Herrington, Amy Easton, Digavalli V. Sivarao, Dawn D. Parker, Rick L. Pieschl, Ping Chen, Guanglin Luo, Omar S. Barnaby, Lorin A. Thompson, Yong-Jin Wu, Andrea McClure, Jason M. Guernon, Amy Newton, Alicia Ng, Clotilde Bourin, Carolyn Diane Dzierba
Publikováno v:
Bioorganic & Medicinal Chemistry. 25:5490-5505
Since zwitterionic benzenesulfonamide Nav1.7 inhibitors suffer from poor membrane permeability, we sought to eliminate this characteristic by replacing the basic moiety with non-basic bicyclic acetals and monocyclic ethers. These efforts led to the d
Autor:
Alicia Ng, Andrea McClure, Chiehying Chang, Fukang Yang, Hyunsoo Park, Yong-Jin Wu, Jason M. Guernon, Jianliang Shi, John E. Macor, Charles F. Albright, Ramkumar Rajamani, Michael K. Ahlijanian, Lorin A. Thompson, Jeremy H. Toyn, Lawrence B. Snyder, Hal A. Lewis, Dan Camac
Publikováno v:
ACS Medicinal Chemistry Letters. 7:271-276
By targeting the flap backbone of the BACE1 active site, we discovered 6-dimethylisoxazole-substituted biaryl aminothiazine 18 with 34-fold improved BACE1 inhibitory activity over the lead compound 1. The cocrystal structure of 18 bound to the active
Autor:
Yong-Jin, Wu, Jason, Guernon, Andrea, McClure, Brian, Venables, Ramkumar, Rajamani, Kevin J, Robbins, Ronald J, Knox, Michele, Matchett, Rick L, Pieschl, James, Herrington, Linda J, Bristow, Nicholas A, Meanwell, Richard, Olson, Lorin A, Thompson, Carolyn, Dzierba
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(5)
Replacement of the piperidine ring in the lead benzenesulfonamide Na
Autor:
Yong-Jin, Wu, Jason, Guernon, Andrea, McClure, Guanglin, Luo, Ramkumar, Rajamani, Alicia, Ng, Amy, Easton, Amy, Newton, Clotilde, Bourin, Dawn, Parker, Kathleen, Mosure, Omar, Barnaby, Matthew G, Soars, Ronald J, Knox, Michele, Matchett, Rick, Pieschl, James, Herrington, Ping, Chen, D V, Sivarao, Linda J, Bristow, Nicholas A, Meanwell, Joanne, Bronson, Richard, Olson, Lorin A, Thompson, Carolyn, Dzierba
Publikováno v:
Bioorganicmedicinal chemistry. 25(20)
Since zwitterionic benzenesulfonamide Na
Autor:
Martin A. Lewis, Louis S. Chupak, Robert G. Gentles, Shuanghua Hu, Min Ding, Yazhong Huang, Xiaofan Zheng, Yuval Blat, Andrea McClure, Ryan Westphal
Publikováno v:
Bioorganicmedicinal chemistry. 24(7)
N-Benzylic-substituted glycine sulfonamides that reversibly inhibit diacylglycerol (DAG) lipases are reported. Detailed herein are the structure activity relationships, profiling characteristics and physico-chemical properties for the first reported
Autor:
Tatiana E. Shelekhin, William P. Esler, Philip Wickens, Lei Wang, Weifeng Tang, Chih-Yuan Chuang, James N. Livingston, Uday Khire, Libing Chen, Philip Coish, Thomas H. Claus, Stephen O'connor, Andrea Mcclure, Laurel Sweet, James A. Kristie, Robert Schoenleber, Stephen J. Gardell, Donald Bierer, Zahra Fathi, Xiao-Gao Liu, Michael Brands, Georgiy Bondar, Wenlang Fu, Brian T. Bloomquist, Alexandros Vakalopoulos, Derek B. Lowe, Joachim Rudolph, Philip D. Ramsden, Lin Yi, Bullock William H, Astrid A. Ortiz, Martin Michels
Publikováno v:
Journal of medicinal chemistry. 50(21)
The peptide hormone ghrelin is the endogenous ligand for the type 1a growth hormone secretagogue receptor (GHS-R1a) and the only currently known circulating appetite stimulant. GHS-R1a antagonism has therefore been proposed as a potential approach fo