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

Bioorg Med Chem Lett

Departamento de Química Orgánica, Laboratorio de Química Farmacéutica, Universidad de Santiago de Compostela, E-15782, Santiago de Compostela, Spain.

Published: September 2007

We describe the synthesis and binding affinities on D(2), 5-HT(2A) and 5-HT(2C) 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.

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http://dx.doi.org/10.1016/j.bmcl.2007.06.045DOI Listing

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