Zobrazeno 1 - 10
of 57
pro vyhledávání: '"Kempf-Grote A"'
Autor:
John T. Randolph, Matthew J. O’Connor, Fei Han, Charles W. Hutchins, Y. Amy Siu, Min Cho, Yunan Zheng, Jonathan A. Hickson, Jana L. Markley, Vlasios Manaves, Mikkel Algire, Kenton A. Baker, Alex M. Chapman, Sujatha M. Gopalakrishnan, Sanjay C. Panchal, Kelly Foster-Duke, DeAnne F. Stolarik, Anita Kempf-Grote, Darby Dammeier, Stacey Fossey, Qi Sun, Chaohong Sun, Yu Shen, Michael J. Dart, Warren M. Kati, Albert Lai, Ari J. Firestone, Michael E. Kort
Publikováno v:
Journal of Medicinal Chemistry. 66:3852-3865
Akademický článek
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Autor:
Andrew J. King, Lee C. Preusser, Anita J Kempf-Grote, Richard A. Nelson, Gary A. Gintant, James S. Polakowski, Kennan C. Marsh, Thomas J Campbell, Bryan F. Cox, Scott W. Mittelstadt
Publikováno v:
Journal of cardiovascular pharmacology. 54(6)
Torcetrapib is a cholesteryl ester transfer protein inhibitor with an undesired response of increasing arterial pressure in humans. Pressor responses to torcetrapib have been demonstrated in multiple preclinical species. However, these studies have n
Autor:
Peter Curzon, Anita J Kempf-Grote, William H. Bunnelle, Michael J. Buckley, Lynne E. Rueter, Michael Meyer, Tino Dyhring, Kennan C. Marsh, Connie R. Faltynek, Jianguo Ji, Philip K. Ahring, David J. Anderson
Publikováno v:
Biochemical pharmacology. 74(8)
5-[(1R,5S)-3,6-Diazabicyclo[3.2.0]heptan-6-yl]nicotinonitrile (A-366833) is a novel nicotinic acetylcholine receptor (nAChR) ligand that binds to the agonist-binding site ([3H]-cytisine) with Ki value of 3.1 nM and exhibits agonist selectivity at alp
Autor:
Xiaofeng Li, Thomas W. von Geldern, Kenton L. Longenecker, James M. Trevillyan, Chunqiu Lai, Kent D. Stewart, Bradley J. Backes, Thomas H. Lubben, Daisy Pireh, Anita J Kempf-Grote, Hing L. Sham, Zhonghua Pei, David W A Beno, Stephen J. Ballaron
Publikováno v:
Journal of medicinal chemistry. 50(8)
Dipeptidyl peptidase IV (DPP4) inhibitors are emerging as a new class of therapeutic agents for the treatment of type 2 diabetes. They exert their beneficial effects by increasing the levels of active glucagon-like peptide-1 and glucose-dependent ins
Autor:
Kenton L. Longenecker, Bradley J. Backes, David W A Beno, James M. Trevillyan, Hing L. Sham, Hana Kopecka, Michael A. Stashko, Gregory Hamilton, Zhonghua Pei, David Madar, Stephen J. Ballaron, Bradley A. Zinker, Candace Black-Schaefer, Thomas H. Lubben, Chunqiu Lai, Thomas W. von Geldern, Anita J Kempf-Grote, Kent D. Stewart, Zhenping Tian, Amanda K Mika
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(7)
A novel series of pyrrolidine-constrained phenethylamines were developed as dipeptidyl peptidase IV (DPP4) inhibitors for the treatment of type 2 diabetes. The cyclohexene ring of lead-like screening hit 5 was replaced with a pyrrolidine to enable pa
Autor:
Thomas H. Lubben, Michael A. Stashko, Glenn A. Reinhart, Amanda K Mika, David Madar, Hing L. Sham, David W A Beno, Xiaofeng Li, Thomas W. von Geldern, Hong Yong, Zhonghua Pei, Bradley A. Zinker, Kent D. Stewart, James M. Trevillyan, Bradley J. Backes, Mathew M. Mulhern, Andrew S. Judd, Anita J Kempf-Grote, Stephen J. Ballaron, Kenton L. Longenecker, Ryan M. Fryer, Lee C. Preusser
Publikováno v:
Journal of medicinal chemistry. 49(22)
Dipeptidyl peptidase IV (DPP4) deactivates glucose-regulating hormones such as GLP-1 and GIP, thus, DPP4 inhibition has become a useful therapy for type 2 diabetes. Optimization of the high-throughput screening lead 6 led to the discovery of 25 (ABT-
Autor:
Daisy Pireh, Hana Kopecka, David W A Beno, James S. Polakowski, Kent D. Stewart, Thomas H. Lubben, James M. Trevillyan, Glenn A. Reinhart, Anita J Kempf-Grote, Richards Steven J, Lakshmi Bhagavatula, Jason A. Segreti, Michael A. Stashko, Paul E. Wiedeman, David Madar, Kenton L. Longenecker, Hing L. Sham, Steven J. Wittenberger, Xiaofeng Li, Heidi Wells, Thomas W. von Geldern, Ryan M. Fryer, Zhonghua Pei, Bradley A. Zinker, Michelle A. Long, Michael G. Fickes, Amanda K Mika, Todd S. Mcdermott, Stevan W. Djuric, Stephen J. Ballaron, Hong Yong
Publikováno v:
Journal of medicinal chemistry. 49(21)
Dipeptidyl peptidase-IV (DPP-IV) inhibitors are poised to be the next major drug class for the treatment of type 2 diabetes. Structure-activity studies of substitutions at the C5 position of the 2-cyanopyrrolidide warhead led to the discovery of pote
Autor:
Akhteruzzaman Molla, Robert J Carrick, Minghua Sun, William E Kohlbrenner, Kent D. Stewart, Krueger Allan C, Chen Zhao, Warren M. Kati, K. C. Marsh, Dale J. Kempf, Kevin R. Steffy, Clarence J. Maring, Anita J Kempf-Grote, Yibo Xu, W. Graeme Laver, Vincent S. Stoll, Darold L. Madigan, Debra Montgomery, Yu-Gui Gu, Hing L. Sham
Publikováno v:
Journal of medicinal chemistry. 48(12)
The structure-activity relationship (SAR) of a novel hydrophobic binding interaction within a subsite of the influenza neuraminidase (NA) active site was characterized and optimized for a series of trisubstituted pyrrolidine inhibitors modified at th
Autor:
Gunawardana Indrani W, K C Marsh, Patrick D. Kilgannon, D L Arendsen, Stewart Ao, B L Cool, Meuth J, D G Fry, G D Zhu, Schaefer, A J Kempf-Grote, S A Boyd, Kifle L, Gregory F. Okasinski, Gallatin Wm
Publikováno v:
Journal of medicinal chemistry. 44(21)
The elevated expression of cell adhesion molecules (CAMs) on the lumenal surface of vascular endothelial cells is a critical early event in the complex inflammatory process. The adhesive interactions of these CAMs that include E-selectin, ICAM-1, and