Search Results - "Roth, Bruce D."

Hepatoselectivity of statins: Design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors by Park, William K.C., Kennedy, Robert M., Larsen, Scott D., Miller, Steve, Roth, Bruce D., Song, Yuntao, Steinbaugh, Bruce A., Sun, Kevin, Tait, Bradley D., Kowala, Mark C., Trivedi, Bharat K., Auerbach, Bruce, Askew, Valerie, Dillon, Lisa, Hanselman, Jeffrey C., Lin, Zhiwu, Lu, Gina H., Robertson, Andrew, Sekerke, Catherine

“…4-Sulfamoyl pyrroles were designed as novel hepatoselective HMG-CoA reductase inhibitors (statins) to reduce myalgia, a statin-induced adverse effect. The…”
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Structure−Activity Relationships and Pharmacokinetic Analysis for a Series of Potent, Systemically Available Biphenylsulfonamide Matrix Metalloproteinase Inhibitors by O'Brien, Patrick M, Ortwine, Daniel F, Pavlovsky, Alexander G, Picard, Joseph A, Sliskovic, Drago R, Roth, Bruce D, Dyer, Richard D, Johnson, Linda L, Man, Chiu Fai, Hallak, Hussein

“…A series of biphenylsulfonamide derivatives of (S)-2-(biphenyl-4-sulfonylamino)-3-methylbutyric acid (5) were prepared and evaluated for their ability to…”
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Synthesis and structure–Activity relationship of 2-amino-3-heteroaryl-quinoxalines as non-peptide, small-Molecule antagonists for interleukin-8 receptor by Li, Jie Jack, Carson, Kenneth G, Trivedi, Bharat K, Yue, Wen Song, Ye, Qing, Glynn, Roberta A, Miller, Steven R, Connor, David T, Roth, Bruce D, Luly, Jay R, Low, Joseph E, Heilig, David J, Yang, Weixing, Qin, Shixin, Hunt, Stephen

“…Interleukin-8 modulation is implicated in many inflammatory and cancer diseases. Starting from a mass-screening hit, the synthesis and structure–activity…”
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Synthesis, Structure−Activity Relationships, and in Vivo Evaluations of Substituted Di-tert-butylphenols as a Novel Class of Potent, Selective, and Orally Active Cyclooxygenase-2 Inhibitors. 1. Thiazolone and Oxazolone Series by Song, Yuntao, Connor, David T, Doubleday, Robert, Sorenson, Roderick J, Sercel, Anthony D, Unangst, Paul C, Roth, Bruce D, Gilbertsen, Richard B, Chan, Kam, Schrier, Denis J, Guglietta, Antonio, Bornemeier, Dirk A, Dyer, Richard D

“…Selective cyclooxygenase-2 (COX-2) inhibitors have been shown to be potent antiinflammatory agents with fewer side effects than currently marketed nonsteroidal…”
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Inhibitors of cholesterol biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-(1H-pyrrol-1-yl)ethyl]-2H-pyran 2-one inhibitors of HMG-CoA reductase. 2. Effects of introducing substituents at positions three and four of the pyrrole nucleus by Roth, Bruce D, Blankley, C. J, Chucholowski, A. W, Ferguson, E, Hoefle, M. L, Ortwine, D. F, Newton, R. S, Sekerke, C. S, Sliskovic, D. R, Wilson, M

“…A series of trans-tetrahydro-4-hydroxy-6-[2-(2,3,4,5-substituted-1H-pyrrol-1-yl) ethyl]-2H-pyran-2-ones and their dihydroxy acids were prepared and tested for…”
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Inhibitors of acyl-CoA:cholesterol acyltransferase. 1. Identification and structure-activity relationships of a novel series of fatty acid anilide hypocholesterolemic agents by Roth, Bruce D, Blankley, C. John, Hoefle, Milton L, Holmes, Ann, Roark, W. Howard, Trivedi, Bharat K, Essenburg, Arnold D, Kieft, Karen A, Krause, Brian R, Stanfield, Richard L

“…A series of fatty acid anilides was prepared, and compounds were tested for their ability to inhibit the enzyme acyl-CoA:cholesterol acyltransferase (ACAT) in…”
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Synthesis, Structure−Activity Relationships, and in Vivo Evaluations of Substituted Di-tert-butylphenols as a Novel Class of Potent, Selective, and Orally Active Cyclooxygenase-2 Inhibitors. 2. 1,3,4- and 1,2,4-Thiadiazole Series by Song, Yuntao, Connor, David T, Sercel, Anthony D, Sorenson, Roderick J, Doubleday, Robert, Unangst, Paul C, Roth, Bruce D, Beylin, Vlad G, Gilbertsen, Richard B, Chan, Kam, Schrier, Denis J, Guglietta, Antonio, Bornemeier, Dirk A, Dyer, Richard D

“…Two isoforms of the cyclooxygenase (COX) enzyme have been identified:  COX-1, which is expressed constitutively, and COX-2, which is induced in inflammation…”
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Novel Nonpeptide CCK-B Antagonists:  Design and Development of Quinazolinone Derivatives as Potent, Selective, and Orally Active CCK-B Antagonists by Padia, Janak K, Field, Mark, Hinton, Joanna, Meecham, Ken, Pablo, Julius, Pinnock, Rob, Roth, Bruce D, Singh, Lakhbir, Suman-Chauhan, Nirmala, Trivedi, Bharat K, Webdale, Louise

“…We have designed a novel series of CCK-B receptor antagonists by combining key pharmacophores, an arylurea moiety of 1 and a quinazolinone ring of 3, from two…”
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Metabolism and Excretion of Atorvastatin in Rats And Dogs by BLACK, A. E, HAYES, R. N, ROTH, B. D, WOO, P, WOOLF, T. F

“…Atorvastatin (AT) is a second-generation potent inhibitor of 3-hydroxy-3-methylglutaryl-CoA reductase, clinically approved for lowering plasma cholesterol…”
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Inhibitors of cholesterol biosynthesis. 1. trans-6-(2-Pyrrol-1-ylethyl)-4-hydroxypyran-2-ones, a novel series of HMG-CoA reductase inhibitors. 1. Effects of structural modifications at the 2- and 5-positions of the pyrrole nucleus by Roth, Bruce D, Ortwine, D. F, Hoefle, M. L, Stratton, C. D, Sliskovic, D. R, Wilson, M. W, Newton, R. S

“…A novel series of trans-6-(2-pyrrol-1-ylethyl)-4-hydroxypyran-2-ones and their dihydroxy acid derivatives were prepared and evaluated for their ability to…”
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ACAT inhibitors: evolution from cholesterol-absorption inhibitors to antiatherosclerotic agents by Roth, Bruce D.

“…Considerable research efforts have focused on the discovery of safe and efficacious acyl-CoA cholesterol acyltransferase (ACAT) inhibitors as…”
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Relationship between tissue selectivity and lipophilicity for inhibitors of HMG-CoA reductase by Roth, Bruce D, Bocan, Thomas M. A, Blankley, C. John, Chucholowski, Alexander W, Creger, Paul L, Creswell, Mark W, Ferguson, Erika, Newton, Roger S, O'Brien, Patrick

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Inhibitors of acyl-CoA:cholesterol acyltransferase. 5. Identification and structure-activity relationships of novel .beta.-keto amides as hypocholesterolemic agents by Augelli-Szafran, Corinne E, Blankley, C. John, Roth, Bruce D, Trivedi, Bharat K, Bousley, Richard F, Essenburg, Arnold D, Hamelehle, Katherine L, Krause, Brian R, Stanfield, Richard L

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Inhibitors of lipoprotein(a) assembly by Sexton, Karen E, Lee, Helen T, Massa, Mark, Padia, Janak, Patt, William C, Liao, Peggy, Pontrello, Jason K, Roth, Bruce D, Spahr, Mark A, Ramharack, Randy

“…Compounds of the general structure A and B were investigated for their activity as lipoprotein(a), [Lp(a)], assembly (coupling) inhibitors. SAR around the…”
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(S)-4-Methyl-2-(methylamino)pentanoic Acid [4,4-Bis(4-fluorophenyl)butyl]amide Hydrochloride, a Novel Calcium Channel Antagonist, Is Efficacious in Several Animal Models of Pain by Song, Yuntao, Bowersox, S. Scott, Connor, David T, Dooley, David J, Lotarski, Susan M, Malone, Thomas, Miljanich, George, Millerman, Elizabeth, Rafferty, Michael F, Rock, David, Roth, Bruce D, Schmidt, Joann, Stoehr, Sally, Szoke, Balazs G, Taylor, Charles, Vartanian, Mark, Wang, Yong-Xiang

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Antiatherosclerotic activity of inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase in cholesterol-fed rabbits: a biochemical and morphological evaluation by Bocan, T M, Mazur, M J, Mueller, S B, Brown, E Q, Sliskovic, D R, O'Brien, P M, Creswell, M W, Lee, H, Uhlendorf, P D, Roth, B D

“…Atherosclerotic lesion development was assessed in the thoracic aorta and chronically denuded iliac-femoral artery of hypercholesterolemic New Zealand White…”
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Inhibitors of Acyl-CoA:Cholesterol O-Acyl Transferase (ACAT) as Hypocholesterolemic Agents. 8. Incorporation of Amide or Amine Functionalities into a Series of Disubstituted Ureas and Carbamates. Effects on ACAT Inhibition in vitro and Efficacy in vivo by O'Brien, Patrick M, Sliskovic, Drago R, Blankley, C. John, Roth, Bruce. D, Wilson, Michael W, Hamelehle, Katherine L, Krause, Brian R, Stanfield, Richard L

“…A series of disubstituted ureas containing amide or amine groups was prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyl…”
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Inhibitors of Acyl-CoA:Cholesterol O-Acyltransferase. Synthesis and Pharmacological Activity of (±)-2-Dodecyl-α-phenyl-N-(2,4,6-trimethoxyphenyl)-2H-tetrazole-5-acetamide and Structurally Related Tetrazole Amide Derivatives by O'Brien, Patrick M, Sliskovic, Drago R, Picard, Joseph A, Lee, Helen T, Purchase, Claude F, Roth, Bruce D, White, Andrew D, Anderson, Maureen, Mueller, Sandra Bak, Bocan, Thomas, Bousley, Richard, Hamelehle, Katherine L, Homan, Reynold, Lee, Peter, Krause, Brian R, Reindel, J. F, Turluck, Daniel

“…A series of tetrazole amide derivatives of (±)-2-dodecyl-α-phenyl-N-(2,4,6-trimethoxyphenyl)-2H-tetrazole-5-acetamide (1) was prepared and evaluated for their…”
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α-Substituted Malonester Amides:  Tools To Define the Relationship between ACAT Inhibition and Adrenal Toxicity by Sliskovic, Drago R, Picard, Joseph A, O'Brien, Patrick M, Liao, Peggy, Roark, W. Howard, Roth, Bruce D, Anderson, Maureen A, Mueller, Sandra Bak, Bocan, Thomas M. A, Bousley, Richard F, Hamelehle, Katherine L, Homan, Reynold, Reindel, James F, Stanfield, Richard L, Turluck, Daniel, Krause, Brian R

“…We prepared a series of α-substituted malonester amides that were evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyl transferase activity in…”
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Inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). 2. Modification of fatty acid anilide ACAT inhibitors: bioisosteric replacement of the amide bond by Roark, W. Howard, Roth, Bruce D, Holmes, Ann, Trivedi, Bharat K, Kieft, Karen A, Essenburg, Arnold D, Krause, Brian R, Stanfield, Richard L

“…In order to further define the structural features necessary for potent inhibition of acyl-coenzyme A:cholesterol acyltransferase (ACAT) in vitro and…”
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