Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Thao, Perry"'
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:
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:
Jeff A, Zablocki, Elfatih, Elzein, Xiaofen, Li, Dmitry O, Koltun, Eric Q, Parkhill, Tetsuya, Kobayashi, Ruben, Martinez, Britton, Corkey, Haibo, Jiang, Thao, Perry, Rao, Kalla, Gregory T, Notte, Oliver, Saunders, Michael, Graupe, Yafan, Lu, Chandru, Venkataramani, Juan, Guerrero, Jason, Perry, Mark, Osier, Robert, Strickley, Gongxin, Liu, Wei-Qun, Wang, Lufei, Hu, Xiao-Jun, Li, Nesrine, El-Bizri, Ryoko, Hirakawa, Kris, Kahlig, Cheng, Xie, Cindy Hong, Li, Arvinder K, Dhalla, Sridharan, Rajamani, Nevena, Mollova, Daniel, Soohoo, Eve-Irene, Lepist, Bernard, Murray, Gerry, Rhodes, Luiz, Belardinelli, Manoj C, Desai
Publikováno v:
Journal of medicinal chemistry. 59(19)
Late sodium current (late I
Autor:
Xiaofen Li, Rao Kalla, Art Gimbel, Thao Perry, Elfatih Elzein, Jeff Zablocki, Ming Yang, Dewan Zeng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1397-1401
A series of N-1 monosubstituted 8-pyrazolyl xanthines have been synthesized and evaluated for their affinity for the adenosine receptors (AdoRs). We have discovered two compounds 18 (CVT-7124) and 28 (CVT-6694) that display good affinity for the A(2B
Autor:
Venkata Palle, Dewan Zeng, Arthur Gimbel, Xiaofen Li, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Rao Kalla, Jeff Zablocki, Tennig Maa
Publikováno v:
Journal of Medicinal Chemistry. 49:3682-3692
Adenosine has been suggested to induce bronchial hyperresponsiveness in asthmatics, which is believed to be an A(2B) adenosine receptor (AdoR) mediated pathway. We hypothesize that a selective, high-affinity A(2B) AdoR antagonist may provide therapeu
Autor:
David Lustig, Elfatih Elzein, Rao Kalla, Xiaofen Li, Dewan Zeng, Art Gimbel, Kwan Leung, Thao Perry, Jeff Zablocki
Publikováno v:
Journal of medicinal chemistry. 51(7)
Recently, we have reported a series of new 1,3-symmetrically (R 1 = R 3) substituted xanthines ( 3 and 4) which have high affinity and selectivity for the human adenosine A 2B receptors (hA(2B)-AdoR). Unfortunately, this class of compounds had poor p
Autor:
Rao Kalla, Xiaofen Li, Thao Perry, Mark Micklatcher, Jeff Zablocki, Yuzhi Wu, Tim Marquart, Yuan Li, Elfatih Elzein, Dewan Zeng
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(1)
A series of new selective, high affinity A(1)-AdoR agonists is reported. Compound 23 that incorporated a carboxylic acid functionality in the 4-position of the pyrazole ring displayed K(iL) value of 1 nM for the A(1)-AdoR and5000-fold selectivity ove
Autor:
Rao V, Kalla, Elfatih, Elzein, Thao, Perry, Xiaofen, Li, Venkata, Palle, Vaibhav, Varkhedkar, Arthur, Gimbel, Tennig, Maa, Dewan, Zeng, Jeff, Zablocki
Publikováno v:
Journal of medicinal chemistry. 49(12)
Adenosine has been suggested to induce bronchial hyperresponsiveness in asthmatics, which is believed to be an A(2B) adenosine receptor (AdoR) mediated pathway. We hypothesize that a selective, high-affinity A(2B) AdoR antagonist may provide therapeu
Autor:
Dengming Xiao, Jia Hao, Piscopio Anthony D, Art Gimbel, Thao Perry, Venkata Palle, Jeff Zablocki, Dewan Zeng, Vaibhav Varkhedkar, Kwan Leung, Rao Kalla, Nancy Chu, Tenning Maa
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(3)
Adenosine has been suggested to play a role in asthma, possibly via activation of A2B adenosine receptors on mast cells and other pulmonary cells. We describe our initial efforts to discover a xanthine based selective A2B AdoR antagonist that resulte