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

We describe the synthesis and binding affinities on D2, 5-HT2A and 5-HT2C receptors of 6-aminomethyl-6,7-dihydro-1H-indazol-4(5H)-ones and 6-aminomethyl-6,7-dihydro-3-methyl-benzo[d]isoxazol-4(5H)-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.