Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Sandra Leitza"'
Autor:
Zhili Xin, Edward B. Reilly, Kennan C. Marsh, Yihong Li, Jeffery R. Huth, J.T. Link, and Peter DeVries, Nathan L. Lubbers, Zhonghua Pei, Sandra Leitza, Thomas W. von Geldern, Yi Gao, Bryan F. Cox, Greg Okasinski, Gang Liu
Publikováno v:
Journal of Medicinal Chemistry. 44:2913-2920
The interaction of LFA-1 and ICAM-1 plays an important role in the cell adhesion process. On the basis of previously reported SAR and structural information on the binding of our p-arylthiocinnamide series to LFA-1, we have identified the cyclic amid
Autor:
Greg Okasinski, Zhonghua Pei, Edward B. Reilly, Sandra Leitza, James T. Link, Bryan K. Sorensen, Gang Liu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:973-976
Diarylsulfide cyclopropylamides were synthesized and evaluated as LFA-1/ICAM-1 interaction antagonists. A substituent pattern was identified which maximized potency and minimized protein binding as exemplified by antagonist 30 (IC 50 =5 nM).
Autor:
Jeffrey R. Huth, Thomas W. von Geldern, Edward T. Olejniczak, Gang Liu, Devries Peter J, Renaldo Mendoza, Stephen W. Fesik, Gregory F. Okasinski, Sandra Leitza, Edward B. Reilly
Publikováno v:
Journal of Medicinal Chemistry. 44:1202-1210
The interaction between leukocyte function-associated antigen-1 (LFA-1) and intracellular adhesion molecule-1 (ICAM-1) has been implicated in inflammatory and immune diseases. Recently, a novel series of p-arylthio cinnamides has been described as po
Autor:
Thomas W. von Geldern, Bach Nguyen, Sandra Leitza, Gang Liu, Mike Gallatin, Zhonghua Pei, and Kerry Fowler, Edward B. Reilly, Mark Ormes, J.T. Link, Gregory F. Okasinski, Kennan C. Marsh
Publikováno v:
Journal of Medicinal Chemistry. 43:4025-4040
The interaction between leukocyte function-associated antigen-1 (LFA-1), a member of the beta(2)-integrin family of adhesion molecules, and intracellular adhesion molecule ICAM-1 (cd54) is thought to play a critical role in the inflammatory process.
Autor:
John M. Brackett, Jeffrey C Hunt, Xiaoxing Qiu, Heidi Seballos, Sandra Leitza, Amit H. Varma, Samar Kundu, Steve Kuemmerlea, Sheng Lou, Kristen L. Cousineau, Gary E. Tegtmeier
Publikováno v:
Journal of Virological Methods. 68:45-55
Immunoassays were developed to determine the seroprevalence of antibody against human GB virus C (GBV-C). The antigenic target in each assay was a 44.6-kDa glycosylated protein representing the first 315 amino acids encoded by the GBV-C E2 gene. Sera
Autor:
Bryan K. Sorensen, Edward B. Reilly, Gang Liu, Zhonghua Pei, Sandra Leitza, James T. Link, Greg Okasinski
Publikováno v:
ChemInform. 32
Diarylsulfide cyclopropylamides were synthesized and evaluated as LFA-1/ICAM-1 interaction antagonists. A substituent pattern was identified which maximized potency and minimized protein binding as exemplified by antagonist 30 (IC 50 =5 nM).
Autor:
Ruth L. Martin, Andrew S. Judd, Sevan Brodjian, Dariusz Wodka, Gilbert Diaz, Lynch John K, Philip R. Kym, Sandra Leitza, Hing L. Sham, Freeman Jennifer C, Mathew M. Mulhern, Gang Zhao, Andrew J. Souers, Christine A. Collins, Sue Swanson, Brian D. Dayton, Rajesh R. Iyengar, Kathryn Houseman, Regina M. Reilly, H. Doug Falls, Ju Gao, Zhi Su
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(4)
The optimization of potent MCHr1 antagonist 1 with respect to improving its in vitro profile by replacement of the 3,4-methylenedioxy phenyl (piperonyl) moiety led to the discovery of 19, a compound that showed excellent MCHr1 binding and functional
Autor:
Ann Mikhail, Sandra Leitza, Gilbert Diaz, Brian D. Dayton, Lynch John K, Robin Shapiro, Kathryn Houseman, Freeman Jennifer C, Philip R. Kym, Dariusz Wodka, Sevan Brodjian, Eugene N. Bush, Ju Gao, Regina M. Reilly, Gary Gintant, Kennan C. Marsh, Mathew M. Mulhern, Andrew S. Judd, Christine A. Collins, Victoria Knourek-Segel, Andrew J. Souers, Lisa E. Hernandez, H. Douglas Falls, James T. Limberis, Rajesh R. Iyengar, Gang Zhao, Hing L. Sham
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(8)
A series of potent 2-carboxychromone-based melanin-concentrating hormone receptor 1 (MCHr1) antagonists were synthesized and evaluated for hERG (human Ether-a-go-go Related Gene) channel affinity and functional blockade. Basic dialkylamine-terminated
Autor:
Sandra Leitza, Thomas W. von Geldern, Thomas J. Sowin, Sheldon Wang, Gary T. Wang, Edward B. Reilly, Robert G. Gentles
Publikováno v:
ChemInform. 36
2-Amino-4-phenyl pyridine and, to a lesser extent, 4-amino-6-phenyl pyrimidine, were established as isosteres of trans-cinnamide moiety. Applying this isosterism to previously reported p-arylthio cinnamides resulted in the identification of 4-amino-6
Autor:
Sandra Leitza, Jeffrey S. McDermott, Katina M Daniell, Bryan F. Cox, Gilbert Diaz, Gary A. Gintant, Zhi Su, Ruth L. Martin
Publikováno v:
Journal of pharmacological and toxicological methods. 50(3)
Introduction: The human ether-a-go-go-related gene (hERG) encodes a potassium channel responsible for the cardiac delayed rectifier current (IKr) involved in ventricular repolarization. Drugs that block hERG have been associated with QT interval prol