dg-041 and Hemorrhage

dg-041 has been researched along with Hemorrhage* in 1 studies

Other Studies

1 other study(ies) available for dg-041 and Hemorrhage

Article	Year
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 an Journal of medicinal chemistry, 2010, Jan-14, Volume: 53, Issue:1 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. Topics: Acrylamides; Blood Coagulation; Drug Discovery; Hemorrhage; Humans; Ligands; Molecular Structure; Platelet Aggregation; Platelet Aggregation Inhibitors; Receptors, Prostaglandin E; Receptors, Prostaglandin E, EP3 Subtype; Stereoisomerism; Structure-Activity Relationship; Sulfones	2010

Article

Year

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 an

Journal of medicinal chemistry, 2010, Jan-14, Volume: 53, Issue:1

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.

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

2010