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Start Over Author "Cort S" Journal bioorganic & medicinal chemistry letters
10 results on '"Cort S"'

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

Author

Cort S. Madsen, Cindy Chen, Donald W. Combs, Jeffrey A. Robl, Charles M. Langevine, David S. Weinstein, Khehyong Ngu, Wen Liu, Shaobin Zhuang, and Timothy W. Harper

Subjects
Male, Stereochemistry, Clinical Biochemistry, Cell, Pharmaceutical Science, CHO Cells, Biochemistry, Isozyme, Rats, Sprague-Dawley, chemistry.chemical_compound, Lipoxygenase, Cricetulus, Cricetinae, Drug Discovery, medicine, Animals, Humans, Imidazole, Lipoxygenase Inhibitors, Molecular Biology, Sulfamide, chemistry.chemical_classification, biology, Organic Chemistry, Imidazoles, In vitro, Rats, medicine.anatomical_structure, Enzyme, chemistry, Enzyme inhibitor, biology.protein, Molecular Medicine
Abstract

A series of 2,4,5-tri-substituted imidazoles has proven to be highly potent in inhibiting mammalian 15-lipoxygenase (15-LO) with excellent selectivity over human isozymes 5- and P-12-LO. Non-symmetrical sulfamides (e.g., 21a–n) were found to be suitable replacements for the earlier arylsulfonamide-containing members of this series (e.g., 2, 14a–p). Several members of these series also demonstrated potent inhibition of human 15-LO in a cell-based assay.

Published
2007
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2. A switch in enantiomer preference between mitochondrial F1F0-ATPase chemotypes

Author

Hossain Monshizadegan, Andrew T. Pudzianowski, Sharon N. Bisaha, Mary F. Malley, Philip D. Stein, Cort S. Madsen, Jack Z. Gougoutas, and Paulina Wang

Subjects
Models, Molecular, Molecular model, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Biochemistry, Drug Discovery, Molecular Biology, chemistry.chemical_classification, Binding Sites, ATP synthase, biology, Organic Chemistry, Absolute configuration, Stereoisomerism, Mitochondria, Enzyme binding, Proton-Translocating ATPases, Enzyme, chemistry, Enzyme inhibitor, biology.protein, Molecular Medicine, Enantiomer, Pharmacophore
Abstract

The preferred absolute configuration of two series of F1F0-ATP synthase inhibitors was determined. Although the configuration of the active enantiomer in each series is different, each series presents the same ‘triaryl’ pharmacophore to the enzyme binding site.

Published
2005
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6. Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase

Author

Weinstein, David S., primary, Liu, Wen, additional, Gu, Zhengxiang, additional, Langevine, Charles, additional, Ngu, Khehyong, additional, Fadnis, Leena, additional, Combs, Donald W., additional, Sitkoff, Doree, additional, Ahmad, Saleem, additional, Zhuang, Shaobin, additional, Chen, Xing, additional, Wang, Feng-Lai, additional, Loughney, Deborah A., additional, Atwal, Karnail S., additional, Zahler, Robert, additional, Macor, John E., additional, Madsen, Cort S., additional, and Murugesan, Natesan, additional

Published
2005
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8. N -[1-Aryl-2-(1-imidazolo)ethyl]-guanidine derivatives as potent inhibitors of the bovine mitochondrial F 1 F 0 ATP hydrolase

Author

Atwal, Karnail S., primary, Ahmad, Saleem, additional, Ding, Charles Z., additional, Stein, Philip D., additional, Lloyd, John, additional, Hamann, Lawrence G., additional, Green, David W., additional, Ferrara, Francis N., additional, Wang, Paulina, additional, Rogers, W.Lynn, additional, Doweyko, Lidia M., additional, Miller, Arthur V., additional, Bisaha, Sharon N., additional, Schmidt, Joan B., additional, Li, Ling, additional, Yost, Kenneth J., additional, Lan, Hsi-Jung, additional, and Madsen, Cort S., additional

Published
2004
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