کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371824 | 981856 | 2012 | 5 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Isoform-selective thiazolo[5,4-b]pyridine S1P1 agonists possessing acyclic amino carboxylate head-groups Isoform-selective thiazolo[5,4-b]pyridine S1P1 agonists possessing acyclic amino carboxylate head-groups](/preview/png/1371824.png)
Replacement of the azetidine carboxylate of an S1P1 agonist development candidate, AMG 369, with a range of acyclic head-groups led to the identification of a novel, S1P3-sparing S1P1 agonist, (−)-2-amino-4-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl)phenyl)-2-methylbutanoic acid (8c), which possessed good in vivo efficacy and pharmacokinetic properties. A 0.3 mg/kg oral dose of 8c produced a statistically significant reduction in blood lymphocyte counts 24 h post-dosing in female Lewis rats.
Replacement of the azetidine carboxylate of an S1P1 agonist development candidate, AMG 369, with a range of acyclic head-groups led to the identification of a novel, S1P3-sparing S1P1 agonist, (−)-2-amino-4-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl)phenyl)-2-methylbutanoic acid (8c), which possessed good in vivo efficacy and pharmacokinetic properties. A 0.3 mg/kg oral dose of 8c produced a statistically significant reduction in blood lymphocyte counts 24 h post-dosing in female Lewis rats.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 4, 15 February 2012, Pages 1779–1783