T. Harper

发表

Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.

S. Sheriff, D. Seiffert, J. Bozarth, 2017, Journal of medicinal chemistry.

Characterization and separation of the arachidonic acid 5-lipoxygenase and linoleic acid omega-6 lipoxygenase (arachidonic acid 15-lipoxygenase) of human polymorphonuclear leukocytes.

K. Austen, R. Lewis, D. Betteridge, 1985, The Journal of biological chemistry.

Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1).

M. Kirby, R. Seethala, A. Nayeem, 2011, Bioorganic & medicinal chemistry letters.

Beta 3 agonists. Part 1: evolution from inception to BMS-194449.

R. Gregg, A. Mathur, T. Waldron, 2001, Bioorganic & medicinal chemistry letters.

BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.

A. Mathur, T. Waldron, K. Dickinson, 2001, Bioorganic & medicinal chemistry letters.

Leukotriene C4 and D4 formation by particulate enzymes.

R. Murphy, B. Jakschik, T. Harper, 1982, The Journal of biological chemistry.

Design and synthesis of 4-substituted benzamides as potent, selective, and orally bioavailable I(Ks) blockers.

A. Mathur, P. Stein, M. Conder, 2001, Journal of Medicinal Chemistry.

Design and synthesis of 4-substituted benzamides as potent, selective, and orally bioavailable IKs blockers

A. Mathur, P. Stein, Mark A. Smith, 2001 .

Metabolism of leukotrienes B4 and C4 in the isolated perfused rat lung.

N. Voelkel, R. Murphy, J. Westcott, 1984, The Journal of biological chemistry.

[4] The 5-lipoxygenase and leukotriene forming enzymes

R. Murphy, B. Jakschik, T. Harper, 1982 .

Identification and functional characterization of leukotriene B4 20-hydroxylase of human polymorphonuclear leukocytes.

K. Austen, R. Murphy, R. Soberman, 1985, Proceedings of the National Academy of Sciences of the United States of America.

Rapid extraction of leukotrienes from biologic fluids and quantitation by high-performance liquid chromatography.

R. Murphy, R. Murphy, S. Metz, 1982, Journal of chromatography.

Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.

S. Sheriff, D. Seiffert, J. Bozarth, 2015, ACS Medicinal Chemistry Letters.

Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency.

P. Lam, S. Sheriff, D. Seiffert, 2017, Bioorganic & medicinal chemistry letters.

Novel phenylalanine derived diamides as Factor XIa inhibitors.

P. Lam, P. Morin, D. Seiffert, 2016, Bioorganic & medicinal chemistry letters.

Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11β-hydroxydehydrogenase 1 (11β-HSD1).

S. Sheriff, R. Seethala, A. Nayeem, 2011, Bioorganic & medicinal chemistry letters.

Metabolism of leukotriene B4 in isolated rat hepatocytes. Identification of a novel 18-carboxy-19,20-dinor leukotriene B4 metabolite.

R. Murphy, T. Harper, M. Garrity, 1986, The Journal of biological chemistry.

Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).

P. Lam, S. Sheriff, A. Mathur, 2017, Journal of medicinal chemistry.

Cardioselective anti-ischemic ATP-sensitive potassium channel openers.

S. Moreland, G. Grover, P. Sleph, 1993, Journal of medicinal chemistry.

Discovery of selective imidazole-based inhibitors of mammalian 15-lipoxygenase: highly potent against human enzyme within a cellular environment.

C. S. Madsen, Shaobin Zhuang, J. Robl, 2007, Bioorganic & medicinal chemistry letters.

Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa

P. Lam, S. Sheriff, D. Seiffert, 2020 .

Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa.

P. Lam, S. Sheriff, D. Seiffert, 2020, Bioorganic & medicinal chemistry letters.

Potent, Orally Bioavailable and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.

P. Lam, S. Sheriff, A. Mathur, 2019, Journal of medicinal chemistry.

Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.

S. Sheriff, D. Seiffert, A. Rendina, 2016, Bioorganic & medicinal chemistry.

Discovery of Potent Protease-Activated Receptor 4 Antagonists with in vivo Antithrombotic Efficacy.

Shana L. Posy, D. Seiffert, Yanou Yang, 2019, Journal of medicinal chemistry.

Gas-chromatographic resolution of enantiomeric secondary alcohols. Stereoselective reductive metabolism of ketones in rabbit-liver cytosol.

J. Gal, D. Devito, T. Harper, 1981, Drug metabolism and disposition: the biological fate of chemicals.

Mass Spectrometry and Eicosanoid Analysis

R. Murphy, T. Harper, 1985 .

Reaction Phenotyping: Current Industry Efforts to Identify Enzymes Responsible for Metabolizing Drug Candidates

P. Brassil, Timothy W. Harper, Patrick J. Brassil, 2008, The AAPS Journal.

1-Aminobenzotriazole, a Known Cytochrome P450 Inhibitor, Is a Substrate and Inhibitor of N-Acetyltransferase

A. D. Rodrigues, P. Marathe, L. Zhang, 2011, Drug Metabolism and Disposition.

Shift in pH of biological fluids during storage and processing: effect on bioanalysis.

A. Fura, Hongjiang Zhang, W. Shyu, 2003, Journal of pharmaceutical and biomedical analysis.

Dansyl glutathione as a trapping agent for the quantitative estimation and identification of reactive metabolites.

Jinping Gan, W Griffith Humphreys, W. Humphreys, 2005, Chemical research in toxicology.

Multiple pathways are involved in the oral absorption of BMS-262084, a tryptase inhibitor, in rats: role of paracellular transport, binding to trypsin, and P-glycoprotein efflux.

S. Chong, A. Marino, R. Morrison, 2005, Journal of pharmaceutical sciences.

Design, synthesis and evaluation of phenethylaminoheterocycles as K(v)1.5 inhibitors.

Huabin Sun, M. Conder, J. Lloyd, 2014, Bioorganic & medicinal chemistry letters.

Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase.

Saleem Ahmad, C. S. Madsen, Xing Chen, 2011, Bioorganic & medicinal chemistry letters.

Triazolo and imidazo dihydropyrazolopyrimidine potassium channel antagonists.

M. Blanar, M. Conder, J. Lloyd, 2013, Bioorganic & medicinal chemistry letters.

Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues.

W. Humphreys, K. Dickinson, R. Seethala, 2008, Bioorganic & medicinal chemistry letters.

Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity.

D. Cheney, Henry H. Gu, E. Iwanowicz, 2002, Journal of medicinal chemistry.

In Silico Prediction of Biliary Excretion of Drugs in Rats Based on Physicochemical Properties

S. Chong, K. He, B. Xin, 2010, Drug Metabolism and Disposition.

Synthesis and structure-activity relationship of 2-adamantylmethyl tetrazoles as potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).

M. Kirby, R. Seethala, A. Nayeem, 2014, Bioorganic & medicinal chemistry letters.

Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor.

David K. Leahy, J. Barrish, M. Kirby, 2017, Journal of medicinal chemistry.

Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1).

S. Sheriff, R. Seethala, A. Nayeem, 2014, ACS Medicinal Chemistry Letters.

Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1).

S. Sheriff, R. Seethala, A. Nayeem, 2018, ACS medicinal chemistry letters.

BMS-201620: a selective beta 3 agonist.

T. Waldron, K. Dickinson, R. George, 2004, Bioorganic & medicinal chemistry letters.

Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.

David S Nirschl, P. Lam, S. Sheriff, 2019, Bioorganic & medicinal chemistry letters.