chiniofon and Atherosclerosis

chiniofon has been researched along with Atherosclerosis* in 1 studies

Other Studies

1 other study(ies) available for chiniofon and Atherosclerosis

Article	Year
2-(4-Chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[H]quinoline-4-carboxylic acid (PSI-697): identification of a clinical candidate from the quinoline salicylic acid series of P-selectin antagonists. Journal of medicinal chemistry, 2007, Jan-11, Volume: 50, Issue:1 P-selectin-PSGL-1 interaction causes rolling of leukocytes on the endothelial cell surface, which subsequently leads to firm adherence and leukocyte transmigration through the vessel wall into the surrounding tissues. P-selectin is upregulated on the surface of both platelets and endothelium in a variety of atherosclerosis-associated conditions. Consequently, inhibition of this interaction by means of a small molecule P-selectin antagonist is an attractive strategy for the treatment of atherosclerosis. High-throughput screening and subsequent analoging had led to the identification of compound 1 as the lead candidate. Herein, we report the continuation of this work and the discovery of a second-generation series, the tetrahydrobenzoquinoline salicylic acids. These compounds have improved pharmacokinetic properties, and a number of them have shown oral efficacy in mouse and rat models of atherogenesis and vascular injury. The lead 31 (PSI-697), is currently in clinical development for the treatment of atherothrombotic vascular events. Topics: Administration, Oral; Animals; Apolipoproteins E; Atherosclerosis; Carotid Stenosis; Dogs; Fibrinolytic Agents; Hydroxyquinolines; Indoles; Leukocyte Rolling; Male; Mice; Mice, Knockout; P-Selectin; Quinolines; Rats; Rats, Sprague-Dawley; Salicylates; Structure-Activity Relationship	2007

Article

Year

2-(4-Chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[H]quinoline-4-carboxylic acid (PSI-697): identification of a clinical candidate from the quinoline salicylic acid series of P-selectin antagonists.

Journal of medicinal chemistry, 2007, Jan-11, Volume: 50, Issue:1

P-selectin-PSGL-1 interaction causes rolling of leukocytes on the endothelial cell surface, which subsequently leads to firm adherence and leukocyte transmigration through the vessel wall into the surrounding tissues. P-selectin is upregulated on the surface of both platelets and endothelium in a variety of atherosclerosis-associated conditions. Consequently, inhibition of this interaction by means of a small molecule P-selectin antagonist is an attractive strategy for the treatment of atherosclerosis. High-throughput screening and subsequent analoging had led to the identification of compound 1 as the lead candidate. Herein, we report the continuation of this work and the discovery of a second-generation series, the tetrahydrobenzoquinoline salicylic acids. These compounds have improved pharmacokinetic properties, and a number of them have shown oral efficacy in mouse and rat models of atherogenesis and vascular injury. The lead 31 (PSI-697), is currently in clinical development for the treatment of atherothrombotic vascular events.

Topics: Administration, Oral; Animals; Apolipoproteins E; Atherosclerosis; Carotid Stenosis; Dogs; Fibrinolytic Agents; Hydroxyquinolines; Indoles; Leukocyte Rolling; Male; Mice; Mice, Knockout; P-Selectin; Quinolines; Rats; Rats, Sprague-Dawley; Salicylates; Structure-Activity Relationship

2007