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Your search keyword '"Georgeta Hategan"' showing total 2 results
Start Over Author "Georgeta Hategan" Journal journal of medicinal chemistry
2 results on '"Georgeta Hategan"'

1. Structure−Activity Relationship Studies Leading to the Identification of (2E)-3-[l-[(2,4-Dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a Potent and Selective Prostanoid EP3 Receptor Antagonist, as a Novel Antiplatelet Agent That Does Not Prolong Bleeding

Author

Margret Thorsteinnsdottir, Alex S. Kiselyov, Gudmundur Sigthorsson, Rama K. Mishra, Jose Ramirez, Peng Yu, Nian Zhou, Jun Zhang, Emmanuel Onua, Mark E. Gurney, Georgeta Hategan, Thorkell Andresson, David E. Zembower, Wayne Zeller, Jasbir Singh, and Alex Polozov

Subjects
Sulfonyl, chemistry.chemical_classification, Stereochemistry, Antagonist, Prostanoid, Chemical synthesis, Adenosine diphosphate, chemistry.chemical_compound, chemistry, Drug Discovery, medicine, Molecular Medicine, Structure–activity relationship, lipids (amino acids, peptides, and proteins), Prostaglandin E2, Pharmacophore, medicine.drug
Abstract

The EP3 receptor on the platelet mediates prostaglandin E2 potentiation of thrombogenic coagonists including collagen and adenosine diphosphate (ADP). A pharmacophore driven approach led to the identification of diverse peri-substituted heterocycles as potent and selective EP3 receptor antagonists. A simultaneous chemical optimization and druglike assessment of prioritized molecules converged on a lead compound 50 (DG-041) that displayed favorable in vitro and functional activities as an inhibitor of human platelet aggregation. This agent is currently in human clinical trials for the treatment of atherothrombosis.

Published
2009

2. Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent that does not prolong bleeding

Author

Jasbir, Singh, Wayne, Zeller, Nian, Zhou, Georgeta, Hategan, Rama K, Mishra, Alex, Polozov, Peng, Yu, Emmanuel, Onua, Jun, Zhang, José L, Ramírez, Gudmundur, Sigthorsson, Margret, Thorsteinnsdottir, Alex S, Kiselyov, David E, Zembower, Thorkell, Andrésson, and Mark E, Gurney

Subjects
Acrylamides, Molecular Structure, Platelet Aggregation, Hemorrhage, Stereoisomerism, Ligands, Structure-Activity Relationship, Drug Discovery, Receptors, Prostaglandin E, EP3 Subtype, Humans, Receptors, Prostaglandin E, Sulfones, Blood Coagulation, Platelet Aggregation Inhibitors
Abstract

The EP(3) receptor on the platelet mediates prostaglandin E(2) potentiation of thrombogenic coagonists including collagen and adenosine diphosphate (ADP). A pharmacophore driven approach led to the identification of diverse peri-substituted heterocycles as potent and selective EP(3) receptor antagonists. A simultaneous chemical optimization and druglike assessment of prioritized molecules converged on a lead compound 50 (DG-041) that displayed favorable in vitro and functional activities as an inhibitor of human platelet aggregation. This agent is currently in human clinical trials for the treatment of atherothrombosis.

Published
2009

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