Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372953 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
The design and synthesis of a new series of high efficacy β2-agonists devoid of the key benzylic alcohol present in previously described highly efficacious β2-agonists is reported. A hypothesis for the unprecedented level of efficacy is proposed based on considerations of β2-adrenoceptor crystal structure, other biophysical data and modeling studies.
Graphical abstractThe design and synthesis of a new series of high efficacy β2-agonists devoid of the key benzylic alcohol present in previously described highly efficacious β2-agonists is reported. A hypothesis for the unprecedented level of efficacy is proposed based on considerations of β2AR crystal structure, other biophysical data and modeling studies.Figure optionsDownload full-size imageDownload as PowerPoint slide