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Your search keyword '"Dutra JK"' showing total 3 results
Start Over Author "Dutra JK" Journal bioorganic medicinal chemistry letters
3 results on '"Dutra JK"'

1. Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors.

Author

Cheng H, Lundy DeMello KM, Li J, Sakya SM, Ando K, Kawamura K, Kato T, Rafka RJ, Jaynes BH, Ziegler CB, Stevens R, Lund LA, Mann DW, Kilroy C, Haven ML, Nimz EL, Dutra JK, Li C, Minich ML, Kolosko NL, Petras C, Silvia AM, and Seibel SB

Subjects
Animals, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Cyclooxygenase 1 metabolism, Cyclooxygenase 2 metabolism, Cyclooxygenase 2 Inhibitors pharmacology, Dogs, Inhibitory Concentration 50, Pyrazoles pharmacology, Structure-Activity Relationship, Anti-Inflammatory Agents, Non-Steroidal chemical synthesis, Cyclooxygenase 2 Inhibitors chemical synthesis, Pyrazoles chemical synthesis
Abstract

The discovery of heteroaryl-phenyl-substituted pyrazole derivatives as canine selective COX-2 inhibitors is described. Structure-activity relationship (SAR) studies of this class of compounds led to the identification of compound 1 which demonstrated a canine whole blood COX-2 inhibitory IC50 of 12 nM and selectivity ratio of COX-1/COX-2 greater than 4000-fold.

Published
2006
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2. Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.

Author

Li J, DeMello KM, Cheng H, Sakya SM, Bronk BS, Rafka RJ, Jaynes BH, Ziegler CB, Kilroy C, Mann DW, Nimz EL, Lynch MP, Haven ML, Kolosko NL, Minich ML, Li C, Dutra JK, Rast B, Crosson RM, Morton BJ, Kirk GW, Callaghan KM, Koss DA, Shavnya A, Lund LA, Seibel SB, Petras CF, and Silvia A

Subjects
Administration, Oral, Animals, Cyclooxygenase 2, Cyclooxygenase 2 Inhibitors, Dogs, Isoenzymes metabolism, Prostaglandin-Endoperoxide Synthases metabolism, Structure-Activity Relationship, Cyclooxygenase Inhibitors administration & dosage, Cyclooxygenase Inhibitors chemistry, Isoenzymes antagonists & inhibitors, Pyridines administration & dosage, Pyridines chemistry
Abstract

Structure-activity relationship (SAR) studies of 2-[3-di(and tri)fluoromethyl-5-arylpyrazol-1-yl]-5-methanesulfonylpyridine derivatives for canine COX enzymes are described. This led to the identification of 12a as a lead candidate for further progression. The in vitro and in vivo activity of 12a for the canine COX-2 enzyme as well as its in vivo efficacy and pharmacokinetic properties in dog are highlighted.

Published
2004
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3. Synthesis and SAR of azalide 3,6-ketal aromatic derivatives as potent Gram-positive and Gram-negative antibacterial agents.

Author

Cheng H, Dirlam JP, Ziegler CB, Lundy KM, Hayashi SF, Kamicker BJ, Dutra JK, Daniel KL, Santoro SL, George DM, Bertsche CD, Sakya SM, and Suarez-Contreras M

Subjects
Animals, Anti-Bacterial Agents pharmacology, Female, Mastitis drug therapy, Mice, Microbial Sensitivity Tests, Staphylococcus aureus drug effects, Structure-Activity Relationship, Anti-Bacterial Agents chemical synthesis, Azithromycin analogs & derivatives, Gram-Negative Bacteria drug effects, Gram-Positive Bacteria drug effects
Abstract

3,6-Ketals of 15-membered azalide pseudoaglycones are a novel series of macrolide antibiotics. The aromatic derivatives of the azalide 3,6-ketals demonstrated potent antibacterial activities against both Gram-positive and Gram-negative bacteria.

Published
2002
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