Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Dmitry Koltun"'
Autor:
Elfatih Elzein, Cindy Hong Li, Daniel Soohoo, Britton Kenneth Corkey, Chandru Venkataramani, Xiao-Jun Li, Manoj C. Desai, Nesrine El-Bizri, Haibo Jiang, Kobayashi Tetsuya, Nevena Mollova, Sridharan Rajamani, Jason K. Perry, Arvinder Dhalla, Thao Perry, Xiaofen Li, Robert G. Strickley, Notte Gregory, Gerry Rhodes, Ryoko Hirakawa, Luiz Belardinelli, Eve-Irene Lepist, Parkhill Eric Q, Jeff Zablocki, Oliver L. Saunders, Lu Yafan, Rao Kalla, Dmitry Koltun, Cheng Xie, Gongxin Liu, Wei-Qun Wang, Kris M. Kahlig, Bernard P. Murray, Michael Graupe, Guerrero Juan A, Martinez Ruben, Mark Osier, Lufei Hu
Publikováno v:
Journal of Medicinal Chemistry. 59:9005-9017
Late sodium current (late INa) is enhanced during ischemia by reactive oxygen species (ROS) modifying the Nav 1.5 channel, resulting in incomplete inactivation. Compound 4 (GS-6615, eleclazine) a novel, potent, and selective inhibitor of late INa, is
Autor:
Elfatih Elzein, Kobayashi Tetsuya, Brian Stafford, Ryoko Hirakawa, Nevena Mollova, Sridharan Rajamani, Belem Avila, Catherine Smith-Maxwell, Thao Perry, Lin Wu, Jennifer Tang, Jeff Zablocki, Xiaofen Li, Wei-Qun Wang, Dmitry Koltun, Parkhill Eric Q, Robert Jiang, Arvinder Dhalla, Luiz Belardinelli
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:3207-3211
We started with a medium throughput screen of heterocyclic compounds without basic amine groups to avoid hERG and β-blocker activity and identified [1,2,4]triazolo[4,3-a]pyridine as an early lead. Optimization of substituents for Late INa current in
Autor:
N. Pagratis, Simon Lebek, Shekeba Ahmadyar, Lars S. Maier, B. Flörchinger, Charlotte M. Lücht, D Tarnowski, Christof Schmid, Julian Mustroph, Stefan Wagner, B. Marchand, Simon Schopka, Luiz Belardinelli, A. Plößl, W.K. Hung, York Zausig, Maria J. Baier, Dmitry Koltun
Publikováno v:
Journal of molecular and cellular cardiology. 118
Rationale Ca/calmodulin-dependent protein kinase II (CaMKII) was shown to increase diastolic sarcoplasmic reticulum (SR) Ca leak, which can result in delayed afterdepolarizations and triggered arrhythmias. Since increased CaMKII expression and activi
Autor:
Leanna Lagpacan, Christopher Allen Ziebenhaus, Bruno Marchand, Elfatih Elzein, Jason K. Perry, Bernard P. Murray, Scott Preston Simonovich, Parkhill Eric Q, Armando G. Villaseñor, WaiLok K. Hung, Nikos Pagratis, Rao Kalla, Jeff Zablocki, Dmitry Koltun, John R. Somoza, Timothy R. Hansen, Ron Aoyama, Thao Perry, Magdeleine Hung, Xiaofen Li
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(3)
We hereby disclose the discovery of inhibitors of CaMKII (7h and 7i) that are highly potent in rat ventricular myocytes, selective against hERG and other off-target kinases, while possessing good CaMKII tissue isoform selectivity (cardiac γ/δ vs. n
Autor:
Serge Karpinski, Sridharan Rajamani, Dmitry Koltun, Wei-Qun Wang, Cathy Smith-Maxwell, Nesrine El-Bizri, Lina Yao, William J. Crumb, Xiao-Jun Li, John C. Shryock, Arvinder Dhalla, Luiz Belardinelli, Lufei Hu, Cindy Hong Li, Gongxin Liu, Ryoko Hirakawa, Lin Wu, Jeff Zablocki
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 344:23-32
Inhibition of cardiac late sodium current (late I(Na)) is a strategy to suppress arrhythmias and sodium-dependent calcium overload associated with myocardial ischemia and heart failure. Current inhibitors of late I(Na) are unselective and can be proa
Autor:
Nevena Mollova, Alexei V. Ivanov, Ian Henderson, Parkhill Eric Q, Jeffrey Chisholm, Kwan Leung, Andrew G. Cole, Sandra A. Brunn, Andrei Glushkov, Dmitry Koltun, Natalya I. Vasilevich, Nathan A. Zautke, Timur Zilbershtein, Jeff Zablocki
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2048-2052
We identified a series of structurally novel SCD (Delta9 desaturase) inhibitors via high-throughput screening and follow-up SAR studies. Modification of the central bicyclic scaffold has proven key to our potency optimization effort. The most potent
Autor:
Kwan Leung, Ken Rehder, Xiaofen Li, Bob Jiang, Marie Nguyen, Timothy A. Marquart, Nancy Chu, Victoria Y. Maydanik, David Lustig, Kevin D. Shenk, Yuan Li, Elfatih Elzein, Reina Natero, Daniel Soohoo, Prabha Ibrahim, Jeff Zablocki, Suresh S. Kerwar, Dmitry Koltun, Jia Hao, Dewan Zeng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:6017-6021
New inhibitors of palmitoyl-CoA oxidation are based on the introduction of nitrogen heterocycles in the ‘Western Portion’ of the molecule. SAR studies led to the discovery of CVT-4325 (shown), a potent FOXi (IC50 = 380 nM rat mitochondria) with f
Publikováno v:
Synthetic Communications. 34:2523-2529
We have developed a simple one‐step synthesis of 2‐chloromethyl‐1,3,4‐oxadiazoles from commercially available acylhydrazides using 1‐chloro‐2,2,2‐trimethoxyethane as a solvent under microwave irradiation.
Publikováno v:
Tetrahedron Letters. 41:2289-2293
The absolute configuration of the stereogenic center at the β-position of a carboxylic acid can be determined via derivatization with chiral benzylic amines [PhCH(Me)NH 2 or 1-NpCH(Me)NH 2 ]. Acids of known configuration and with a variety of β-sub
Autor:
Thomas E. Goodwin, James R. Vyvyan, Michael L. Guyer, Thomas R. Hoye, Elizabeth G. Jacobs, Sheryl D. Debenham, Jennifer L. Green, David M. Cousins, Dmitry Koltun
Publikováno v:
The Journal of Organic Chemistry. 63:4485-4488