Synthesis and binding affinity of new pyrazole and isoxazole derivatives as potential atypical antipsychotics

Abstract We describe the synthesis and binding affinities on D 2 , 5-HT 2A and 5-HT 2C receptors of 6-aminomethyl-6,7-dihydro-1 H -indazol-4(5 H )-ones and 6-aminomethyl-6,7-dihydro-3-methyl-benzo[ d ]isoxazol-4(5 H )-ones, as conformationally constrained butyrophenone analogues. One of the new compounds showed good in vitro binding features, and a Meltzer’s ratio characteristic of an atypical antipsychotic profile.