11 research outputs found
Identification of 5H-chromeno[3,4-c]pyridine and 6H-isochromeno[3,4-c]pyridine derivatives as potent and selective dual ROCK inhibitors
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Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies
No full textMesenchymal Stem Cells Improve Medullary Inflammation and Fibrosis after Revascularization of Swine Atherosclerotic Renal Artery Stenosis
No full textDiscovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1<i>H</i>)‑one as the P2′ Moiety
No full textStructure–activity
relationship optimization of phenylalanine
P1′ and P2′ regions with a phenylimidazole core resulted
in a series of potent FXIa inhibitors. Introducing 4-hydroxyquinolin-2-one
as the P2′ group enhanced FXIa affinity and metabolic stability.
Incorporation of an <i>N</i>-methyl piperazine amide group
to replace the phenylalanine improved both FXIa potency and aqueous
solubility. Combination of the optimization led to the discovery of
FXIa inhibitor <b>13</b> with a FXIa <i>K</i><sub>i</sub> of 0.04 nM and an aPTT EC<sub>2<i>x</i></sub> of
1.0 μM. Dose-dependent efficacy (EC<sub>50</sub> of 0.53 μM)
was achieved in the rabbit ECAT model with minimal bleeding time prolongation
An additive dripping technique using diphenyl ether for tuning perovskite crystallization for high-efficiency solar cells
No full textThe Superior Mesenteric Artery: From Syndrome in the Young to Vascular Atherosclerosis in the Old
No full textMircrining the injured heart with stem cell-derived exosomes: an emerging strategy of cell-free therapy
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