کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376736 | 981964 | 2006 | 4 صفحه PDF | دانلود رایگان |
A series of potent inhibitors of the sodium hydrogen exchanger-1 (NHE-1) is described. Structure–activity relationships identified the 3-methyl-4-fluoro analog 9t as a highly potent (IC50 = 0.0065 μM) and selective (NHE-2/NHE-1 = 1400) non-acylguanidine NHE-1 inhibitor. Pharmacokinetic studies showed that compound 9t has an oral bioavailability of 52% and a plasma half life of 1.5 h in rats. Because of its promising potency, selectivity, and a good pharmacokinetic profile, compound 9t was selected for further studies.
A series of potent inhibitors of the sodium hydrogen exchanger-1 (NHE-1) is described. Structure–activity relationships identified the 3-methyl-4-fluoro analog 9t as a highly potent (IC50 = 0.0065 μM) and selective (NHE-2/NHE-1 = 1400) non-acylguanidine NHE-1 inhibitor. Pharmacokinetic studies showed that compound 9t has an oral bioavailability of 52% and a plasma half life of 1.5 h in rats.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 18, 15 September 2006, Pages 4796–4799