Descoberta de novos protótipos N-fenilpiperazínicos heteroarilazólicos candidatos a fármacos antipsicóticos atípicos
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Data
2010
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Resumo
This work describes the discovery of new N-phenylpiperazine prototypes belonging to pyrazole series,
i.e. LASSBio-579 (10a), or to 1,2,3-triazole series, represented by LASSBio-581 (10c), which were designed from
the structural simplification of the atypical antipsychotic drug clozapine (8). The evaluation of the affinity and
intrinsic activity profiles of LASSBio-579 and LASSBio-581 indicate its ability to bind dopamine receptors from
D 2 -like family, acting as pre-synaptic agonists. Additionally, the investigation of the antipsychotic properties of
these two prototypes in behavioral models has confirmed its effectiveness, which is also dependent on the
modulation of serotoninergic receptors 5-HT 2A and 5-HT 1A . The pronounced antipsychotic effect evidenced for
these N-phenylpiperazine derivatives through in vivo pharmacological assays confirmed their importance as
new neuroactive drug-candidate prototypes for the treatment of schizophrenia.
Descrição
Palavras-chave
N-phenylpiperazine, Drug design, Pyrazole, Multitarget drugs, 1,2,3-triazole, Antipsychotic drugs, N-fenilpiperazina;, Planejamento de fármacos, Pirazola, Fármacos multirreceptores, 1,2,3-triazol, Fármacos antipsicóticos
Citação
Fraga, C. A. M. et al. Descoberta de novos protótipos N-fenilpiperazínicos heteroarilazólicos candidatos a fármacos antipsicóticos atípicos. Revista Virtual de Química, Niterói, v. 2, n. 1, p. 28-37, 2010.