Design, synthesis and pharmacological evaluation of efficacy selective β2 adrenoceptor agonists

Asthma involves constriction or obstruction of the airways and causes morbidity and mortality worldwide. To treat these conditions, patients are often prescribed β2 adrenoceptor agonists (β2AR). The caveat of current approved drugs is that these compounds can also activate the β1AR. Activation of the β1AR, increases heart rate and force of contraction. This project aims to develop an efficacy selective β2AR agonist Analogues of the naturally occurring β2AR agonist, S1319, and the highly selective β1AR antagonist CGP 20712A were synthesised and Structure-activity relationship studied. The results of these studies facilitated the rational design of the efficacy selective β2AR agonist.