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10 results on '"Mertzman, Michael"'

2. Use of benzofuran for concomitant protection of aldehyde and phenol groups in the preparation of mycophenolic acid analogues

Author

Fardis, Maria, Mertzman, Michael, Thomas, William, Kirschberg, Thorsten, Collins, Nicole, Polniaszek, Richard, and Watkins, William J.

Subjects
Phenolic resins -- Research, Chemical synthesis, Biological sciences, Chemistry
Abstract

An exploration was carried out about the use of a benzofuran to mask phenol and arylacetaldehyde moieties simultaneously in the synthesis of analogues of mycophenolic acid (MPA). Benzofuran provided a stable and easily handled intermediate for the preparation of unnatural derivatives at the C-6 position of MPA.

Published
2006

3. Identification of N‑Methyl Nicotinamide and N‑Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2).

Author

Moslin, Ryan, Zhang, Yanlei, Wrobleski, Stephen T., Lin, Shuqun, Mertzman, Michael, Spergel, Steven, Tokarski, John S., Strnad, Joann, Gillooly, Kathleen, McIntyre, Kim W., Zupa-Fernandez, Adriana, Cheng, Lihong, Sun, Huadong, Chaudhry, Charu, Huang, Christine, D'Arienzo, Celia, Heimrich, Elizabeth, Yang, Xiaoxia, Muckelbauer, Jodi K., and Chang, ChiehYing

Published
2019
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4. Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.

Author

Spergel, Steven H., Mertzman, Michael E., Kempson, James, Guo, Junqing, Stachura, Sylwia, Haque, Lauren, Lippy, Jonathan S., Zhang, Rosemary F., Galella, Michael, Pitt, Sidney, Shen, Guoxiang, Fura, Aberra, Gillooly, Kathleen, McIntyre, Kim W., Tang, Vicky, Tokarski, John, Sack, John S., Khan, Javed, Carter, Percy H., and Barrish, Joel C.

Published
2019
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5. Discovery of GS-9669, a ThumbSite II Non-Nucleoside Inhibitor of NS5B for the Treatment of Genotype1 Chronic Hepatitis C Infection.

Author

Lazerwith, Scott E., Lew, Willard, Zhang, Jennifer, Morganelli, Philip, Liu, Qi, Canales, Eda, Clarke, Michael O., Doerffler, Edward, Byun, Daniel, Mertzman, Michael, Ye, Hong, Chong, Lee, Xu, Lianhong, Appleby, Todd, Chen, Xiaowu, Fenaux, Martijn, Hashash, Ahmad, Leavitt, Stephanie A., Mabery, Eric, and Matles, Mike

Published
2014
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8. Practical olefin hydroamination with nitroarenes.

Author

Jinghan Gui, Chung-Mao Pan, Ying Jin, Tian Qin, Lo, Julian C., Lee, Bryan J., Spergel, Steven H., Mertzman, Michael E., Pitts, William J., La Cruz, Thomas E., Schmidt, Michael A., Darvatkar, Nitin, Natarajan, Swaminathan R., and Baran, Phil S.

Subjects
*ALKENES, *HYDROAMINATION, *NITROAROMATIC compounds, *BIOCHEMICAL substrates, *SECONDARY amines, *CHEMOSELECTIVITY, *FUNCTIONAL groups, *AROMATIC amines
Abstract

The synthesis and functionalization of amines are fundamentally important in a vast range of chemical contexts.We present an amine synthesis that repurposes two simple feedstock building blocks: olefins and nitro(hetero)arenes. Using readily available reactants in an operationally simple procedure, the protocol smoothly yields secondary amines in a formal olefin hydroamination. Because of the presumed radical nature of the process, hindered amines can easily be accessed in a highly chemoselective transformation. A screen of more than 100 substrate combinations showcases tolerance of numerous unprotected functional groups such as alcohols, amines, and even boronic acids. This process is orthogonal to other aryl amine syntheses, such as the Buchwald-Hartwig, Ullmann, and classical amine-carbonyl reductive aminations, as it tolerates aryl halides and carbonyl compounds. [ABSTRACT FROM AUTHOR]

Published
2015
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9. Novel, potent, and orally bioavailable phosphinic acid inhibitors of the hepatitis C virus NS3 protease

Author

Clarke, Michael O., Chen, Xiaowu, Cho, Aesop, Delaney, William E., Doerffler, Edward, Fardis, Maria, Ji, Mingzhe, Mertzman, Michael, Pakdaman, Rowchanak, Pyun, Hyun-Jun, Rowe, Tanisha, Yang, Cheng Y., Sheng, X. Christopher, and Kim, Choung U.

Subjects
*BIOMEDICAL materials, *PHOSPHINIC acid, *CHEMICAL inhibitors, *HEPATITIS C virus, *SERINE proteinases, *CARBOXYLIC acids, *PHARMACOKINETICS, *CONSTRAINTS (Physics), *MACROCYCLIC compounds
Abstract

Abstract: A potent and novel class of product-like inhibitors of the HCV NS3 protease was discovered by employing a phosphinic acid as a carboxylate isostere. The replicon activity and pharmacokinetic profile of this series of compounds was optimized by exploring the substitution of the phosphinic acid, as well as conformationally constraining these compounds through macrocyclization. The syntheses and preliminary biological evaluation of these phosphinic acids is described. [Copyright &y& Elsevier]

Published
2011
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10. Discovery of GS-9256: A novel phosphinic acid derived inhibitor of the hepatitis C virus NS3/4A protease with potent clinical activity

Author

Sheng, X. Christopher, Casarez, Anthony, Cai, Ruby, Clarke, Michael O., Chen, Xiaowu, Cho, Aesop, Delaney, William E., Doerffler, Edward, Ji, Mingzhe, Mertzman, Michael, Pakdaman, Rowchanak, Pyun, Hyung-Jung, Rowe, Tanisha, Wu, Qiaoyin, Xu, Jie, and Kim, Choung U.

Subjects
*VIRAL disease treatment, *PHARMACEUTICAL research, *PHOSPHINIC acid, *HEPATITIS C virus, *PROTEASE inhibitors, *DRUG synergism, *PHARMACOKINETICS
Abstract

Abstract: A potent and novel class of phosphinic acid derived product-like inhibitors of the HCV NS3/4A protease was discovered previously. Modification of the phosphinic acid and quinoline heterocycle led to GS-9256 with potent cell-based activity and favorable pharmacokinetic parameters. Based on these attributes, GS-9256 was advanced to human clinical trial as a treatment for chronic infection with genotype 1 HCV. [Copyright &y& Elsevier]

Published
2012
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