Cell-based and in-silico studies on the high intrinsic activity of two boron-containing salbutamol derivatives at the human β2-adrenoceptor

Design, synthesis and in vitro evaluatio

Design, synthesis and in vitro evaluation of (R)-4-(2-(tert-butylamino)-1-hydroxyethyl)-2-(hydroxymethyl)phenyl hydrogen phenylboronate: A novel salbutamol derivative with high intrinsic efficacy on the β2 adrenoceptor

✍ Marvin A. Soriano-Ursúa; José Correa-Basurto; Ignacio Valencia-Hernández; Marcos 📂 Article 📅 2010 🏛 Elsevier Science 🌐 English ⚖ 746 KB

We tested a set of boron containing arylethanolamine derivatives on the human and guinea pig β(2) adrenoceptor (β(2)AR) 3-D structures by docking methodology. The compound with the highest affinity based on docking analysis, (R)-4-(2-(tert-butylamino)-1-hydroxyethyl)-2-(hydroxymethyl)phenyl hydrogen