Design driven HtL: The discovery and synthesis of new high efficacy β2-agonists

Abstract The design and synthesis of a new series of high efficacy β 2 - agonists devoid of the key benzylic alcohol present in previously described highly efficacious β 2 - agonists is reported. A hypothesis for the unprecedented level of efficacy is proposed based on considerations of β 2 -adrenoceptor crystal structure, other biophysical data and modeling studies.