Employing the dopamine autoreceptor agonist (-)-3-PPP (3) as well as the ch
olinergic receptor ligands 4 and 5 as lead compounds the 3-pyrrolidinylisox
azoles 2a,b as well as its optical antipodes ent-2a,b were synthesized from
(R)-aspartic acid (6) and (S)-aspartic acid (ent-6), respectively. Pharmac
ological properties of the target compounds were evaluated employing dopami
ne D2 receptor binding studies and functional experiments on muscarinic M2
receptors.