Search Results - "Trivedi, Bharat K"

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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Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors by Pfefferkorn, Jeffrey A., Song, Yuntao, Sun, Kuai-Lin, Miller, Steven R., Trivedi, Bharat K., Choi, Chulho, Sorenson, Roderick J., Bratton, Larry D., Unangst, Paul C., Larsen, Scott D., Poel, Toni-Jo, Cheng, Xue-Min, Lee, Chitase, Erasga, Noe, Auerbach, Bruce, Askew, Valerie, Dillon, Lisa, Hanselman, Jeffrey C., Lin, Zhiwu, Lu, Gina, Robertson, Andrew, Olsen, Karl, Mertz, Thomas, Sekerke, Catherine, Pavlovsky, Alexander, Harris, Melissa S., Bainbridge, Graeme, Caspers, Nicole, Chen, Huifen, Eberstadt, Matthias

“…This manuscript describes the design and synthesis of a series of N-iso-propyl pyrrole-based inhibitors of HMG-CoA reductase for the treatment of…”
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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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Discovery of novel hepatoselective HMG-CoA reductase inhibitors for treating hypercholesterolemia: A bench-to-bedside case study on tissue selective drug distribution by Pfefferkorn, Jeffrey A., Litchfield, John, Hutchings, Richard, Cheng, Xue-Min, Larsen, Scott D., Auerbach, Bruce, Bush, Mark R., Lee, Chitase, Erasga, Noe, Bowles, Daniel M., Boyles, David C., Lu, Gina, Sekerke, Catherine, Askew, Valerie, Hanselman, Jeffrey C., Dillon, Lisa, Lin, Zhiwu, Robertson, Andrew, Olsen, Karl, Boustany, Carine, Atkinson, Karen, Goosen, Theunis C., Sahasrabudhe, Vaishali, Chupka, Jonathan, Duignan, David B., Feng, Bo, Scialis, Renato, Kimoto, Emi, Bi, Yi-An, Lai, Yurong, El-Kattan, Ayman, Bakker-Arkema, Rebecca, Barclay, Paul, Kindt, Erick, Le, Vu, Mandema, Jaap W., Milad, Mark, Tait, Bradley D., Kennedy, Robert, Trivedi, Bharat K., Kowala, Mark

“…The design of drugs with selective tissue distribution can be an effective strategy for enhancing efficacy and safety, but understanding the translation of…”
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Discovery of pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase by Bratton, Larry D., Auerbach, Bruce, Choi, Chulho, Dillon, Lisa, Hanselman, Jeffrey C., Larsen, Scott D., Lu, Gina, Olsen, Karl, Pfefferkorn, Jeffrey A., Robertson, Andrew, Sekerke, Catherine, Trivedi, Bharat K., Unangst, Paul C.

“…Novel substituted pyrroles containing lower alkyl groups and polar functionality were shown to be potent hepatoselective inhibitors of HMG-CoA reductase. In an…”
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Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors by Pfefferkorn, Jeffrey A., Choi, Chulho, Song, Yuntao, Trivedi, Bharat K., Larsen, Scott D., Askew, Valerie, Dillon, Lisa, Hanselman, Jeffrey C., Lin, Zhiwu, Lu, Gina, Robertson, Andrew, Sekerke, Catherine, Auerbach, Bruce, Pavlovsky, Alexander, Harris, Melissa S., Bainbridge, Graeme, Caspers, Nicole

“…Using structure-based design, a novel series of conformationally restricted, pyrrole-based inhibitors of HMG-CoA reductase inhibitors were discovered. Using…”
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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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Inhibitors of acyl-CoA:cholesterol acyltransferase. 4. A novel series of urea ACAT inhibitors as potential hypocholesterolemic agents by Trivedi, Bharat K, Holmes, Ann, Stoeber, Terri L, Blankley, C. John, Roark, W. Howard, Picard, Joseph A, Shaw, Mary K, Essenburg, Arnold D, Stanfield, Richard L, Krause, Brian R

“…We have synthesized a series of N-phenyl-N'-aralkyl and N-phenyl-N'-(1-phenylcycloalkyl)ureas as inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT)…”
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Attenuation of diet‐induced atherosclerosis in rabbits with a highly selective 15‐lipoxygenase inhibitor lacking significant antioxidant properties by Sendobry, Sandra M., Cornicelli, Joseph A., Welch, Kathryn, Bocan, Thomas, Tait, Bradley, Trivedi, Bharat K., Colbry, Norman, Dyer, Richard D., Feinmark, Steven J., Daugherty, Alan

“…15‐Lipoxygenase (15‐LO) has been implicated in the pathogenesis of atherosclerosis because of its localization in lesions and the many biological activities…”
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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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Discovery of highly potent and selective benzyloxybenzyl-based peroxisome proliferator-activator receptor (PPAR) δ agonists by Bratton, Larry D., Filzen, Gary F., Geyer, Andrew, Hoffman, Jennifer K., Lu, Gina, Pulaski, Jim, Trivedi, Bharat K., Unangst, Paul C., Xu, Xiangyang

“…A series of 1,4-benzyloxybenzylsulfanylaryl carboxylic acids were prepared and their activities for PPAR receptor subtypes (α, δ, and γ) with potential…”
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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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Second Generation “Peptoid” CCK-B Receptor Antagonists:  Identification and Development of N-(Adamantyloxycarbonyl)-α-methyl-(R)-tryptophan Derivative (CI-1015) with an Improved Pharmacokinetic Profile by Trivedi, Bharat K, Padia, Janak K, Holmes, Ann, Rose, Steven, Wright, D. Scott, Hinton, Joanna P, Pritchard, Martyn C, Eden, Jon M, Kneen, Clare, Webdale, Louise, Suman-Chauhan, Nirmala, Boden, Phil, Singh, Lakhbir, Field, Mark J, Hill, David

“…We have previously described the design and development of CI-988, a peptoid analogue of CCK-4 with excellent binding affinity and selectivity for the CCK-B…”
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Inhibitors of Acyl-CoA:Cholesterol Acyltransferase (ACAT). 7. Development of a Series of Substituted N-Phenyl-N'-[(1-phenylcyclopentyl)methyl]ureas with Enhanced Hypocholesterolemic Activity by Trivedi, Bharat K, Purchase, Terri Stoeber, Holmes, Ann, Augelli-Szafran, Corinne E, Essenburg, Arnold D, Hamelehle, Katherine L, Stanfield, Richard L, Bousley, Richard F, Krause, Brian R

“…We recently described our initial structure-activity relationship (SAR) studies on a series of N-phenyl-N'-aralkyl- and N-phenyl-N'-(1-phenylcycloalkyl)ureas…”
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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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N6-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)ethyl]adenosine and its uronamide derivatives. Novel adenosine agonists with both high affinity and high selectivity for the adenosine A2 receptor by Bridges, Alexander J, Bruns, Robert F, Ortwine, Daniel F, Priebe, Steven R, Szotek, Deedee L, Trivedi, Bharat K

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[1,2,4]Triazolo[4,3-a]quinoxalin-4-amines: a new class of A1 receptor selective adenosine antagonists by Trivedi, Bharat K, Bruns, Robert F

“…Several [1,2,4]triazolo[4,3-a]quinoxalines that were reported as antidepressants in the patent literature were found to possess moderate affinity for the…”
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C2,N6-Disubstituted adenosines: synthesis and structure-activity relationships by Trivedi, Bharat K, Bruns, Robert F

“…Extracellular adenosine receptors have been divided into two major subtypes, called A1 and A2. Substitution of the adenosine molecule with appropriate groups…”
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Development of a practical synthesis of novel, pyrrole-based HMG-CoA reductase inhibitors by Pfefferkorn, Jeffrey A., Bowles, Daniel M., Kissel, William, Boyles, David C., Choi, Chulho, Larsen, Scott D., Song, Yuntao, Sun, Kuai-Lin, Miller, Steven R., Trivedi, Bharat K.

“…This paper describes the development of an efficient and scalable second generation synthesis of novel, pyrrole-based HMG-CoA reductase inhibitors. Compound 1…”
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Stereoselective antitumor properties in the Lewis Lung carcinoma model using bis(morpholinomethyl) derivatives of tricyclic bis(dioxopiperazines) by Witiak, Donald T, Trivedi, Bharat K, Schmid, Franz A

“…Geometric isomers of 2,11-bis(morpholinomethyl)tetrahydrodipyrazino[1,2-a:2',1'-c]pyraz ine-1, 3,10,12-(2H,4H,9H,11H)-tetrone (3 and 4) and the parent…”
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