Search Results - "Liu, Eddie C."

Dissecting the activation of thienopyridines by cytochromes P450 using a pharmacodynamic assay in vitro by Abell, Lynn M, Liu, Eddie C-K

“…The thienopyridine antiplatelet drugs, such as ticlopidine, clopidogrel, and prasugrel, require activation by cytochromes P450 in vivo to effectively block…”
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Antithrombotic and hemostatic effects of a small molecule factor XIa inhibitor in rats by Schumacher, William A., Seiler, Steven E., Steinbacher, Thomas E, Stewart, Anne B., Bostwick, Jeffrey S., Hartl, Karen S., Liu, Eddie C., Ogletree, Martin L.

“…The effect of inhibiting activated blood coagulation factor XIa was determined in rat models of thrombosis and hemostasis. BMS-262084 is an irreversible and…”
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Design, Structure−Activity Relationships, X-ray Crystal Structure, and Energetic Contributions of a Critical P1 Pharmacophore: 3-Chloroindole-7-yl-Based Factor Xa Inhibitors by Shi, Yan, Sitkoff, Doree, Zhang, Jing, Klei, Herbert E, Kish, Kevin, Liu, Eddie C.-K, Hartl, Karen S, Seiler, Steve M, Chang, Ming, Huang, Christine, Youssef, Sonia, Steinbacher, Thomas E, Schumacher, William A, Grazier, Nyeemah, Pudzianowski, Andrew, Apedo, Atsu, Discenza, Lorell, Yanchunas, Joseph, Stein, Philip D, Atwal, Karnail S

“…An indole-based P1 moiety was incorporated into a previously established factor Xa inhibitor series. The indole group was designed to hydrogen-bond with the…”
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Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors by Shi, Yan, O’Connor, Stephen P., Sitkoff, Doree, Zhang, Jing, Shi, Mengxiao, Bisaha, Sharon N., Wang, Ying, Li, Chi, Ruan, Zheming, Michael Lawrence, R., Klei, Herbert E., Kish, Kevin, Liu, Eddie C.-K., Seiler, Steve M., Schweizer, Liang, Steinbacher, Thomas E., Schumacher, William A., Robl, Jeffrey A., Macor, John E., Atwal, Karnail S., Stein, Philip D.

“…The design, synthesis and SAR of a novel class of valerolactam-based arylsulfonamides as potent and selective FXa inhibitors is reported. The…”
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Aroylguanidine-based factor Xa inhibitors: The discovery of BMS-344577 by Shi, Yan, Li, Chi, O’Connor, Stephen P., Zhang, Jing, Shi, Mengxiao, Bisaha, Sharon N., Wang, Ying, Sitkoff, Doree, Pudzianowski, Andrew T., Huang, Christine, Klei, Herbert E., Kish, Kevin, Yanchunas, Joseph, Liu, Eddie C.-K., Hartl, Karen S., Seiler, Steve M., Steinbacher, Thomas E., Schumacher, William A., Atwal, Karnail S., Stein, Philip D.

“…We report the design and synthesis of a novel class of N,N′-disubstituted aroylguanidine-based lactam derivatives as potent and orally active FXa inhibitors…”
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Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors by Shi, Yan, Zhang, Jing, Shi, Mengxiao, O’Connor, Stephen P., Bisaha, Sharon N., Li, Chi, Sitkoff, Doree, Pudzianowski, Andrew T., Chong, Saeho, Klei, Herbert E., Kish, Kevin, Yanchunas, Joseph, Liu, Eddie C.-K., Hartl, Karen S., Seiler, Steve M., Steinbacher, Thomas E., Schumacher, William A., Atwal, Karnail S., Stein, Philip D.

“…The N,N′-disubstituted cyanoguanidine is an excellent bioisostere of the thiourea and ketene aminal functional groups. We report the design and synthesis of a…”
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Synthesis and evaluation of acylguanidine FXa inhibitors by O’Connor, Stephen P., Atwal, Karnail, Li, Chi, Liu, Eddie C.-K., Seiler, Steven M., Shi, Mengxiao, Shi, Yan, Stein, Philip D., Wang, Ying

“…A series of acylguanidine derivatives were prepared and investigated as inhibitors of Factor Xa (FXa). These compounds were made by guanidine acylation with…”
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Development and validation of a platelet calcium flux assay using a fluorescent imaging plate reader by Liu, Eddie C.-K., Abell, Lynn M.

“…Calcium signaling in platelets is an important physiological response to various aggregation stimuli. Loading platelets with various fluorescent dyes and…”
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Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors by Shi, Yan, Sitkoff, Doree, Zhang, Jing, Han, Wei, Hu, Zilun, Stein, Philip D., Wang, Ying, Kennedy, Lawrence J., O’Connor, Stephen P., Ahmad, Saleem, Liu, Eddie C.-K., Seiler, Steve M., Lam, Patrick Y.S., Robl, Jeffrey A., Macor, John E., Atwal, Karnail S., Zahler, Robert

“…The design and synthesis of a novel class of amino(methyl) pyrrolidine-based sulfonamides as potent and selective FXa inhibitors is reported. The amino(methyl)…”
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The Discovery of Sulfonamide Endothelin Antagonists and the Development of the Orally Active ETA Antagonist 5-(Dimethylamino)-N-(3,4-dimethyl-5- isoxazolyl)-1-naphthalenesulfonamide by Stein, Philip D, Hunt, John T, Floyd, David M, Moreland, Suzanne, Dickinson, Kenneth E. J, Mitchell, Caroline, Liu, Eddie C.-K, Webb, Maria L, Murugesan, Natesan

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Biphenylsulfonamide Endothelin Receptor Antagonists. Part 3: Structure–Activity Relationship of 4′-Heterocyclic Biphenylsulfonamides by Murugesan, Natesan, Gu, Zhengxiang, Stein, Philip D., Spergel, Steven, Bisaha, Sharon, Liu, Eddie C.-K., Zhang, Rongan, Webb, Maria L., Moreland, Suzanne, Barrish, Joel C.

“…A number of 4′-heterocyclic biphenylsulfonamide derivatives, formally derived from BMS-193884 ( 1) by replacing the oxazole ring with other heterocyclic rings,…”
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Biphenylsulfonamide Endothelin Receptor Antagonists. 4. Discovery of N-[[2‘-[[(4,5-Dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1‘-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), A Highly Potent and Orally Active ETA Selective Antagonist by Murugesan, Natesan, Gu, Zhengxiang, Spergel, Steven, Young, Marian, Chen, Ping, Mathur, Arvind, Leith, Leslie, Hermsmeier, Mark, Liu, Eddie C.-K, Zhang, Rongan, Bird, Eileen, Waldron, Tom, Marino, Anthony, Koplowitz, Barry, Humphreys, W. Griffith, Chong, Saeho, Morrison, Richard A, Webb, Maria L, Moreland, Suzanne, Trippodo, Nick, Barrish, Joel C

“…We have previously disclosed the selective ETA receptor antagonist N-(3,4-dimethyl-5-isoxazolyl)-4‘-(2-oxazolyl)[1,1‘-biphenyl]-2-sulfonamide (1, BMS-193884)…”
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Discovery and Structure-Activity Relationships of Sulfonamide ETA-Selective Antagonists by Stein, Philip D, Floyd, David M, Bisaha, Sharon, Dickey, Joyce, Girotra, Ravindar N, Gougoutas, Jack Z, Kozlowski, Michael, Lee, Ving G, Liu, Eddie C.-K

“…Random screening of compounds in an ETA receptor binding assay led to the discovery of a class of benzenesulfonamide ligands. Optimization led to the…”
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Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors by Shi, Yan, Zhang, Jing, Stein, Philip D., Shi, Mengxiao, O’Connor, Stephen P., Bisaha, Sharon N., Li, Chi, Atwal, Karnail S., Bisacchi, Gregory S., Sitkoff, Doree, Pudzianowski, Andrew T., Liu, Eddie C., Hartl, Karen S., Seiler, Steven M., Youssef, Sonia, Steinbacher, Thomas E., Schumacher, William A., Rendina, Alan R., Bozarth, Jeffrey M., Peterson, Tara L., Zhang, Ge, Zahler, Robert

“…N, N′-Disubstituted ketene aminals are good bioisosteres of thiourea functional groups. We report the design and synthesis of a novel class of ketene…”
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Biphenylsulfonamide Endothelin Receptor Antagonists. 2. Discovery of 4‘-Oxazolyl Biphenylsulfonamides as a New Class of Potent, Highly Selective ETA Antagonists by Murugesan, Natesan, Gu, Zhengxiang, Stein, Philip D, Spergel, Steven, Mathur, Arvind, Leith, Leslie, Liu, Eddie C.-K, Zhang, Rongan, Bird, Eileen, Waldron, Tom, Marino, Anthony, Morrison, Richard A, Webb, Maria L, Moreland, Suzanne, Barrish, Joel C

“…The synthesis and structure−activity relationship (SAR) studies of a series of 4‘-oxazolyl-N-(3,4-dimethyl-5-isoxazolyl)[1,1‘-biphenyl]-2-sulfonamide…”
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Biphenylsulfonamide Endothelin Antagonists:  Structure−Activity Relationships of a Series of Mono- and Disubstituted Analogues and Pharmacology of the Orally Active Endothelin Antagonist 2‘-Amino-N- (3,4-dimethyl-5-isoxazolyl)-4‘-(2-methylpropyl)[1,1‘-biphenyl]-2-sulfonamide (BMS-187308) by Murugesan, Natesan, Gu, Zhengxiang, Stein, Philip D, Bisaha, Sharon, Spergel, Steve, Girotra, Ravi, Lee, Ving G, Lloyd, John, Misra, Raj N, Schmidt, Joan, Mathur, Arvind, Stratton, Leslie, Kelly, Yolanda F, Bird, Eileen, Waldron, Tom, Liu, Eddie C.-K, Zhang, Rongan, Lee, Helen, Serafino, Randy, Abboa-Offei, Benoni, Mathers, Parker, Giancarli, Mary, Seymour, Andrea Ann, Webb, Maria L, Moreland, Suzanne, Barrish, Joel C, Hunt, John T

“…Substitution at the ortho position of N-(3,4-dimethyl-5-isoxazolyl) benzenesulfonamide led to the identification of the biphenylsulfonamides as a novel series…”
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Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist by Murugesan, Natesan, Gu, Zhengxiang, Spergel, Steven, Young, Marian, Chen, Ping, Mathur, Arvind, Leith, Leslie, Hermsmeier, Mark, Liu, Eddie C-K, Zhang, Rongan, Bird, Eileen, Waldron, Tom, Marino, Anthony, Koplowitz, Barry, Humphreys, W Griffith, Chong, Saeho, Morrison, Richard A, Webb, Maria L, Moreland, Suzanne, Trippodo, Nick, Barrish, Joel C

“…We have previously disclosed the selective ET(A) receptor antagonist N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-oxazolyl)[1,1'-biphenyl]-2-sulfonamide (1, BMS-193884)…”
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Mutational Analysis of the Endothelin Type A Receptor (ETA):  Interactions and Model of the Selective ETA Antagonist BMS-182874 with the Putative ETA Receptor Binding Cavity by Webb, Maria L, Patel, Pramathesh S, Rose, Patricia M, Liu, Eddie C. K, Stein, Philip D, Barrish, Joel, Lach, David A, Stouch, Terry, Fisher, Susan M, Hadjilambris, Ophelia, Lee, Helen, Skwish, Stephen, Dickinson, Kenneth E. J, Krystek, Stanley R

“…Endothelin (ET) receptor antagonism is a potential therapeutic intervention in the treatment of vascular diseases. To elucidate the mechanism of antagonist−ET…”
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Binding of 125I-endothelin-1 and 125I-endothelin-3 in rabbit saphenous vein: evidence for an atypical ET binding component by Liu, E C, Monshizadegan, H, Chao, C C, Lynch, J, Fisher, S M, Rose, P M, Webb, M L

“…Recent investigations have confirmed the presence of vasoconstrictory endothelinB (ETB) receptors in several tissues, including the rabbit saphenous vein…”
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Site-specific biotinylation. A novel approach and its application to endothelin-1 analogs and PTH-analog by Natarajan, S, Festin, S M, Hedberg, A, Liu, E C, Floyd, D M, Hunt, J T

“…We have developed an expeditious method for the incorporation of the biotinylaminocaproyl moiety on the epsilon-amino group of a lysine residue within a…”
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