pai-039 and Carotid-Artery-Thrombosis

pai-039 has been researched along with Carotid-Artery-Thrombosis* in 1 studies

Other Studies

1 other study(ies) available for pai-039 and Carotid-Artery-Thrombosis

Article	Year
Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization. Journal of medicinal chemistry, 2004, Jul-01, Volume: 47, Issue:14 Indole oxoacetic acid derivatives were prepared and evaluated for in vitro binding to and inactivation of human plasminogen activator inhibitor-1 (PAI-1). SAR based on biochemical, physiological, and pharmacokinetic attributes led to identification of tiplaxtinin as the optimal selective PAI-1 inhibitor. Tiplaxtinin exhibited in vivo oral efficacy in two different models of acute arterial thrombosis. The remarkable preclinical safety and metabolic stability profiles of tiplaxtinin led to advancing the compound to clinical trials. Topics: Administration, Oral; Animals; Biological Availability; Carotid Artery Thrombosis; Coronary Thrombosis; Dogs; Drug Design; Drug Evaluation, Preclinical; Humans; Indoleacetic Acids; Indoles; Plasminogen Activator Inhibitor 1; Rats; Serine Proteinase Inhibitors; Structure-Activity Relationship	2004

Article

Year

Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization.

Journal of medicinal chemistry, 2004, Jul-01, Volume: 47, Issue:14

Indole oxoacetic acid derivatives were prepared and evaluated for in vitro binding to and inactivation of human plasminogen activator inhibitor-1 (PAI-1). SAR based on biochemical, physiological, and pharmacokinetic attributes led to identification of tiplaxtinin as the optimal selective PAI-1 inhibitor. Tiplaxtinin exhibited in vivo oral efficacy in two different models of acute arterial thrombosis. The remarkable preclinical safety and metabolic stability profiles of tiplaxtinin led to advancing the compound to clinical trials.

Topics: Administration, Oral; Animals; Biological Availability; Carotid Artery Thrombosis; Coronary Thrombosis; Dogs; Drug Design; Drug Evaluation, Preclinical; Humans; Indoleacetic Acids; Indoles; Plasminogen Activator Inhibitor 1; Rats; Serine Proteinase Inhibitors; Structure-Activity Relationship

2004