کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1357177 | 981209 | 2005 | 12 صفحه PDF | دانلود رایگان |
A novel series of dipeptidyl α-ketoamide derivatives with amphiphile was designed and synthesized as water-soluble calpain inhibitors. The introduction of amphiphiles at the P3 site increased water solubility without loss of membrane permeability and provided the oral available inhibitors. Extension of the ethylene glycol chain at the P3 site led to an improvement in persistence of plasma levels. In particular, introduction of a combination of a diethylene glycol methyl ether moiety at the P3 site, a phenylalanine residue at the P1 site and a cyclopropyl moiety at the P′ site was the most effective modification for an increase in plasma drug exposure.
A novel series of dipeptidyl α-ketoamide derivatives with amphiphile was designed and synthesized as water-soluble calpain inhibitors.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 13, Issue 14, 15 July 2005, Pages 4473–4484