Discovery of 2-[1-(4-chlorophenyl)cyclopropyl]-3-hydroxy-8-(trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury.
第一作者:
Adrian,Huang
第一单位:
Pfizer Global Research and Development, 200 Cambridge Park Drive, Cambridge, Massachusetts 02140, USA.
作者:
医学主题词
投药, 口服(Administration, Oral);动物(Animals);Caco-2细胞(Caco-2 Cells);颈动脉损伤(Carotid Artery Injuries);细胞膜通透性(Cell Membrane Permeability);狗(Dogs);药物稳定性(Drug Stability);人类(Humans);羟喹啉类(Hydroxyquinolines);白细胞滚动(Leukocyte Rolling);成束猴(Macaca fascicularis);小鼠(Mice);小鼠, 近交C57BL(Mice, Inbred C57BL);微粒体, 肝(Microsomes, Liver);模型, 分子(Models, Molecular);P选择素(P-Selectin);狒狒属(Papio);大鼠(Rats);大鼠, Sprague-Dawley(Rats, Sprague-Dawley);水杨酸盐类(Salicylates);溶解度(Solubility);构效关系(Structure-Activity Relationship);静脉血栓形成(Venous Thrombosis)
DOI
10.1021/jm9013696
PMID
20718494
发布时间
2012-11-15
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