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Your search keyword '"James B. Kramer"' showing total 4 results
Start Over Author "James B. Kramer" Journal journal of medicinal chemistry
4 results on '"James B. Kramer"'

1. Difluoromethylene at the γ-Lactam α-Position Improves 11-Deoxy-8-aza-PGE

Author

Stephen D, Barrett, Melissa C, Holt, James B, Kramer, Bradlee, Germain, Chi S, Ho, Fred L, Ciske, Andrei, Kornilov, Joseph M, Colombo, Adam, Uzieblo, James P, O'Malley, Thomas A, Owen, Adam J, Stein, and Maria I, Morano

Subjects
Binding Sites, Pyrrolidines, Lactams, Molecular Structure, CHO Cells, Molecular Docking Simulation, Cricetulus, Models, Chemical, Heptanoic Acids, Receptors, Prostaglandin E, EP3 Subtype, Animals, Humans, Quantum Theory, Alprostadil, Caco-2 Cells, Receptors, Prostaglandin E, EP4 Subtype
Abstract

A series of small-molecule full agonists of the prostaglandin E

Published
2019

2. Inhibition of E-selectin-, ICAM-1-, and VCAM-1-mediated cell adhesion by benzo[b]thiophene-, benzofuran-, indole-, and naphthalene-2-carboxamides: identification of PD 144795 as an antiinflammatory agent

Author

Khatana Ss, G. C. N. Okonkwo, K. Imre, Roderick J. Sorenson, Mark E. Lesch, Clifford D. Wright, James B. Kramer, Mark A. Ferin, David T. Connor, and Diane H. Boschelli

Subjects
Indoles, Magnetic Resonance Spectroscopy, Neutrophils, Intercellular Adhesion Molecule-1, Administration, Oral, Vascular Cell Adhesion Molecule-1, Thiophenes, Naphthalenes, chemistry.chemical_compound, Mice, Drug Discovery, E-selectin, Cell Adhesion, Animals, Humans, Benzofuran, VCAM-1, Cell adhesion, Cells, Cultured, Benzofurans, ICAM-1, Bicyclic molecule, biology, Cell adhesion molecule, Chemistry, Tumor Necrosis Factor-alpha, Anti-Inflammatory Agents, Non-Steroidal, Molecular biology, Amides, biology.protein, Molecular Medicine, Endothelium, Vascular, E-Selectin, Cell Adhesion Molecules
Abstract

It was previously reported that 3-alkoxybenzo[b]thiophene-2-carboxamides exemplified by 1, 5-methoxy-3-(1-methylethoxy)benzo[b]thiophene-2-carboxamide, decreased the adherence of neutrophils to activated endothelial cells by inhibiting the upregulation of the adhesion molecules E-selectin and ICAM-1 on the surface of the endothelium. This finding is extended here to a series of 3-thiobenzo[b]thiophene-2-carboxamides and also heterocyclic analogs of 1, including benzofurans, indoles, and naphthalenes. The compounds that inhibited the expression of E-selectin and ICAM-1 had the same effect on the expression of VCAM-1. PD 144795, 5-methoxy-3-(1-methylethoxy)benzo[b]thiophene-2-carboxamide 1-oxide (44), the sulfoxide analog of 1, was orally active in several models of inflammation. The in vitro and in vivo activity of PD 144795 resided predominately in the S-enantiomer.

Published
1995

3. 3-Alkoxybenzo[b]thiophene-2-carboxamides as inhibitors of neutrophil-endothelial cell adhesion

Author

David T. Connor, Diane H. Boschelli, Mark A. Ferin, Denis J. Schrier, James B. Kramer, Mark E. Lesch, and Clifford D. Wright

Subjects
Chemistry, Neutrophils, Neutrophile, Anti-Inflammatory Agents, Non-Steroidal, Motility, Tetrazoles, Biological activity, Adhesion, Thiophenes, Molecular biology, In vitro, Rats, Endothelial stem cell, chemistry.chemical_compound, Structure-Activity Relationship, Biochemistry, In vivo, Drug Discovery, Thiophene, Cell Adhesion, Molecular Medicine, Animals, Humans, Endothelium, Vascular
Published
1994

4. A novel prodrug of an impermeant inhibitor of 3-deoxy-D-manno-2-octulosonate cytidylyltransferase has antibacterial activity

Author

James B. Kramer, William Rosenbrook, D. W. Norbeck, David J. Grampovnik, and Paul A. Lartey

Subjects
Salmonella typhimurium, Chemical Phenomena, Esterification, biology, Cytidylyltransferase, Sugar Acids, Prodrug, biology.organism_classification, Nucleotidyltransferases, Anti-Bacterial Agents, carbohydrates (lipids), Chemistry, chemistry.chemical_compound, chemistry, Biochemistry, Biosynthesis, Drug Discovery, Molecular Medicine, Prodrugs, Hydroxymethyl, Antibacterial activity, Bacteria, Intracellular, Antibacterial agent
Abstract

Although 8-amino-2,6-anhydro-3,8-dideoxy-D-glycero-D-talo-octonic acid (2) is a potent inhibitor of 3-deoxy-D-manno-octulosonate cytidylyltransferase (CMP-KDO synthetase), it is unable to reach its cytoplasmic target and is therefore inactive as an antibacterial agent. However, esterification of 2 with 8-(hydroxymethyl)-1-naphthyl methyl disulfide (8) generates a prodrug (12), which gains entry into bacterial cells. Intracellular reduction of the disulfide leads to a rapid, intramolecular, displacement of the acid 2, which then inhibits the growth of Gram-negative bacteria by interfering with the biosynthesis of lipopolysaccharide.

Published
1989
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