Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Parkhill Eric Q"'
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:
Koltun, Dmitry O., Parkhill, Eric Q., Kalla, Rao, Perry, Thao D., Elzein, Elfatih, Li, Xiaofen, Simonovich, Scott P., Ziebenhaus, Christopher, Hansen, Timothy R., Marchand, Bruno, Hung, WaiLok K., Lagpacan, Leanna, Hung, Magdeleine, Aoyama, Ron G., Murray, Bernard P., Perry, Jason K., Somoza, John R., Villaseñor, Armando G., Pagratis, Nikos, Zablocki, Jeff A.
Publikováno v:
In Bioorganic & Medicinal Chemistry Letters 1 February 2018 28(3):541-546
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:
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:
Koltun, Dmitry O., Parkhill, Eric Q., Elzein, Elfatih, Kobayashi, Tetsuya, Notte, Gregory T., Kalla, Rao, Jiang, Robert H., Li, Xiaofen, Perry, Thao D., Avila, Belem, Wang, Wei-Qun, Smith-Maxwell, Catherine, Dhalla, Arvinder K., Rajamani, Sridharan, Stafford, Brian, Tang, Jennifer, Mollova, Nevena, Belardinelli, Luiz, Zablocki, Jeff A.
Publikováno v:
In Bioorganic & Medicinal Chemistry Letters 1 July 2016 26(13):3202-3206
Autor:
Koltun, Dmitry O., Parkhill, Eric Q., Elzein, Elfatih, Kobayashi, Tetsuya, Jiang, Robert H., Li, Xiaofen, Perry, Thao D., Avila, Belem, Wang, Wei-Qun, Hirakawa, Ryoko, Smith-Maxwell, Catherine, Wu, Lin, Dhalla, Arvinder K., Rajamani, Sridharan, Mollova, Nevena, Stafford, Brian, Tang, Jennifer, Belardinelli, Luiz, Zablocki, Jeff A.
Publikováno v:
In Bioorganic & Medicinal Chemistry Letters 1 July 2016 26(13):3207-3211
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
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Autor:
Ian Henderson, Jeffrey Chisholm, Nathan A. Zautke, Melanie Boze, Jia Hao, Timur Zilbershtein, Natalya I. Vasilevich, Dmitry Koltun, Jeff Zablocki, Elena Mayboroda, Andrei Glushkov, Sandra A. Brunn, Nancy Chu, Parkhill Eric Q, Kwan Leung, Andrew G. Cole, Nevena Mollova
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(11)
We discovered a structurally novel SCD (Delta9 desaturase) inhibitor 4a (CVT-11,563) that has 119 nM potency in a human cell-based (HEPG2) SCD assay and selectivity against Delta5 and Delta6 desaturases. This compound has 90% oral bioavailability (ra
Autor:
Zablocki, Jeff A., Elzein, Elfatih, Li, Xiaofen, Koltun, Dmitry O., Parkhill, Eric Q., Tetsuya Kobayashi, Martinez, Ruben, Corkey, Britton, Haibo Jiang, Perry, Thao, Kalla, Rao, Notte, Gregory T., Saunders, Oliver, Graupe, Michael, Lu, Yafan, Venkataramani, Chandru, Guerrero, Juan, Perry, Jason, Osier, Mark, Strickley, Robert
Publikováno v:
Journal of Medicinal Chemistry; Oct2016, Vol. 59 Issue 19, p9005-9017, 13p