Search Results - "Buckman, Brad O."

Novel Small Molecule Inhibitors of 3-Phosphoinositide-dependent Kinase-1 by Feldman, Richard I., Wu, James M., Polokoff, Mark A., Kochanny, Monica J., Dinter, Harald, Zhu, Daguang, Biroc, Sandra L., Alicke, Bruno, Bryant, Judi, Yuan, Shendong, Buckman, Brad O., Lentz, Dao, Ferrer, Mike, Whitlow, Marc, Adler, Marc, Finster, Silke, Chang, Zheng, Arnaiz, Damian O.

“…The phosphoinositide 3-kinase/3-phosphoinositide-dependent kinase 1 (PDK1)/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumor…”
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A novel inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa) - part II: enhancement of both exogenous and endogenous fibrinolysis in animal models of thrombosis by Wang, Yi-Xin, da Cunha, Valdeci, Vincelette, Jon, Zhao, Lei, Nagashima, Mariko, Kawai, Kohichi, Yuan, Shendong, Emayan, Kumar, Islam, Imadul, Hosoya, Junko, Sullivan, Mark E, Dole, William P, Morser, John, Buckman, Brad O, Vergona, Ronald

“…We have discovered a novel small-molecule TAFIa inhibitor, BX 528, which is potent, highly selective against other carboxypeptidases and safe. The present…”
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A novel P2Y(12) adenosine diphosphate receptor antagonist that inhibits platelet aggregation and thrombus formation in rat and dog models by Wang, Yi-Xin, Vincelette, Jon, da Cunha, Valdeci, Martin-McNulty, Baby, Mallari, Cornell, Fitch, Richard M, Alexander, Serene, Islam, Imadul, Buckman, Brad O, Yuan, Shendong, Post, Joseph M, Subramanyam, Babu, Vergona, Ronald, Sullivan, Mark E, Dole, William P, Morser, John, Bryant, Judi

“…Irreversible platelet inhibitors, such as aspirin and clopidogrel, have limited anti-thrombotic efficacy in the clinic due to their bleeding risk. We have…”
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HCV NS5B polymerase inhibitors 1: Synthesis and in vitro activity of 2-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-1-hydroxynaphthalene derivatives by Wang, Guangyi, He, Yanzhen, Sun, Jun, Das, Debasis, Hu, Mougang, Huang, Jianhua, Ruhrmund, Donald, Hooi, Lisa, Misialek, Shawn, Ravi Rajagopalan, P.T., Stoycheva, Antitsa, Buckman, Brad O., Kossen, Karl, Seiwert, Scott D., Beigelman, Leonid

“…Synthesis of 2-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-1-hydroxynaphthalene derivatives and in vitro anti-HCV activity are reported…”
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A novel inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) - part I: pharmacological characterization by Wang, Yi-Xin, Zhao, Lei, Nagashima, Mariko, Vincelette, Jon, Sukovich, Drew, Li, Weiwei, Subramanyam, Babu, Yuan, Shendong, Emayan, Kumar, Islam, Imadul, Hrvatin, Paul, Bryant, Judi, Light, David R, Vergona, Ronald, Morser, John, Buckman, Brad O

“…We have discovered a novel small-molecule (3-phosphinoylpropionic acid) inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa), BX 528,…”
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HCV NS5B polymerase inhibitors 3: Synthesis and in vitro activity of 3-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-4-hydroxy-2H-quinolizin-2-one derivatives by Wang, Guangyi, Zhang, Laiguo, Wu, Xiaomin, Das, Debasis, Ruhrmund, Donald, Hooi, Lisa, Misialek, Shawn, Ravi Rajagopalan, P.T., Buckman, Brad O., Kossen, Karl, Seiwert, Scott D., Beigelman, Leonid

“…Synthesis of 3-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-4-hydroxy-2H-quinolizin-2-one derivatives and in vitro anti-HCV activity are reported…”
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Total Synthesis of Covalent Cysteine Protease Inhibitor N‑Desmethyl Thalassospiramide C and Crystallographic Evidence for Its Mode of Action by Fournier, Jeremy, Chen, Karen, Mailyan, Artur K, Jackson, Jeffrey J, Buckman, Brad O, Emayan, Kumar, Yuan, Shendong, Rajagopalan, Ravi, Misialek, Shawn, Adler, Marc, Blaesse, Michael, Griessner, Andreas, Zakarian, Armen

“…A total synthesis of N-desmethyl thalassospiramide C, a unique strained macrocyclic proteobacterial depsipeptide, enabled a detailed crystallographic study of…”
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Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis by Islam, Imadul, Yuan, Shendong, West, Christopher W., Adler, Marc, Bothe, Ulrich, Bryant, Judi, Chang, Zheng, Chu, Kieu, Emayan, Kumar, Gualtieri, Giovanna, Ho, Elena, Light, David, Mallari, Cornell, Morser, John, Phillips, Gary, Schaefer, Caralee, Sukovich, Drew, Whitlow, Marc, Chen, Deborah, Buckman, Brad O.

“…[Display omitted] •Design and synthesis of benzylamine based selective and orally available inhibitors of uPA has been described.•Prior knowledge of SAR has…”
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Reversible, orally available ADP receptor (P2Y12) antagonists Part I: Hit to lead process by Islam, Imadul, Yuan, Shendong, Wei, Robert G., Xu, Wei, Morrissey, Michael, Mohan, Raju, Zheng, Dewan, DiMella, Andrea, Dunning, Laura, Snider, Michael, Subramanyam, Babu, Tseng, Jih-Lie, Bryant, Judi A., Buckman, Brad O.

“…[Display omitted] •A hit to lead process to discover reversible, orally available ADP receptor (P2Y12) antagonists has been described.•Parallel synthesis,…”
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Recent advances in drug discovery of benzothiadiazine and related analogs as HCV NS5B polymerase inhibitors by Das, Debasis, Hong, Jian, Chen, Shu-Hui, Wang, Guangyi, Beigelman, Leonid, Seiwert, Scott D., Buckman, Brad O.

“…Hepatitis C virus (HCV) is a major health burden, with an estimated 170 million chronically infected individuals worldwide, and a leading cause of liver…”
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Synthesis and biological evaluation of menthol-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) by Ye, Bin, Bauer, Shawn, Buckman, Brad O., Ghannam, Ameen, Griedel, Brian D., Khim, Seock-Kyu, Lee, Wheeseong, Sacchi, Karna L., Shaw, Kenneth J., Liang, Amy, Wu, Qingyu, Zhao, Zuchun

“…Compound 1 was identified by high throughput screening as a novel PAI-1 inhibitor. Optimization of the B and C-segments of 1 resulted in a series of…”
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Design, Synthesis, and Activity of a Novel Series of Factor Xa Inhibitors:  Optimization of Arylamidine Groups by Phillips, Gary, Guilford, William J, Buckman, Brad O, Davey, David D, Eagen, Keith A, Koovakkat, Sunil, Liang, Amy, McCarrick, Meg, Mohan, Raju, Ng, Howard P, Pinkerton, Michael, Subramanyam, Babu, Ho, Elena, Trinh, Lan, Whitlow, Marc, Wu, Shung, Xu, Wei, Morrissey, Michael M

“…A novel series of diaryloxypyridines have been designed as selective nanomolar factor Xa (fXa) inhibitors for use as anticoagulants. In this paper, we describe…”
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Manganese(III)-based asymmetric oxidative free-radical cyclization of unsaturated .beta.-keto sulfoxides by Snider, Barry B, Wan, Barbara Yu Fong, Buckman, Brad O, Foxman, Bruce M

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Solvent effects on manganese(III)-based oxidative free-radical cyclizations: ethanol and acetic acid by Snider, Barry B, Merritt, John E, Dombroski, Mark A, Buckman, Brad O

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3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa) by Islam, Imadul, Bryant, Judi, May, Karen, Mohan, Raju, Yuan, Shendong, Kent, Lorraine, Morser, John, Zhao, Lei, Vergona, Ron, White, Kathy, Adler, Marc, Whitlow, Marc, Buckman, Brad O.

“…A novel series of cyclic potent, selective, small molecule, thiol-based inhibitors of activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) are…”
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HCV NS5B polymerase inhibitors 2: Synthesis and in vitro activity of (1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl) azolo[1,5-a]pyridine and azolo[1,5-a]pyrimidine derivatives by Wang, Guangyi, Lei, Huoxing, Wang, Xiaofang, Das, Debasis, Hong, Jian, Mackinnon, Colin H., Coulter, Thomas S., Montalbetti, Christian A.G.N., Mears, Richard, Gai, Xinjie, Bailey, Sarah E., Ruhrmund, Donald, Hooi, Lisa, Misialek, Shawn, Rajagopalan, P.T. Ravi, Cheng, Robert K.Y., Barker, John J., Felicetti, Brunella, Schönfeld, Dorian L., Stoycheva, Antitsa, Buckman, Brad O., Kossen, Karl, Seiwert, Scott D., Beigelman, Leonid

“…Synthesis of (1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl) azolo[1,5-a]pyridine and azolo[1,5-a]pyrimidine derivatives and in vitro anti-HCV activity are…”
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Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors by Buckman, Brad O., Chou, Yuo-Ling, McCarrick, Meg, Liang, Amy, Lentz, Dao, Mohan, Raju, Morrissey, Michael M., Shaw, Kenneth J., Trinh, Lan, Light, David R.

“…Reductive amination followed by acylation of polymer-linked formyl aryl amidines generate combinatorial libraries of aryl amidines. Potent small molecule…”
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Termination of manganese(III)-based oxidative free-radical cyclizations by addition to nitriles. Formation of cyclopentanones and cyclohexanones by Snider, Barry B, Buckman, Brad O

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Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin by Whitlow, Marc, Arnaiz, Damain O., Buckman, Brad O., Davey, David D., Griedel, Brain, Guilford, William J., Koovakkat, Sunil K., Liang, Amy, Mohan, Raju, Phillips, Gary B., Seto, Marian, Shaw, Kenneth J., Xu, Wei, Zhao, Zuchun, Light, David R., Morrissey, Michael M.

“…Factor Xa is a serine protease which activates thrombin (factor IIa) and plays a key regulatory role in the blood‐coagulation cascade. Factor Xa is, therefore,…”
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Solution-phase parallel synthesis of benzoxazines using a polymer-supported carbodiimide by Buckman, Brad O., Morrissey, Michael M., Mohan, Raju

“…A diverse library of 2-aminobenzoxazines 3 has been synthesized using a two step approach. Addition of anthranilic acids to isocyanates affords ureas 2 that…”
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