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Synthesis and biological evaluation of promising heterocyclic analogues of aripiprazole with potential antipsychotic activity

Grant number: 14/12896-1
Support Opportunities:Scholarships in Brazil - Scientific Initiation
Effective date (Start): September 01, 2014
Effective date (End): August 31, 2016
Field of knowledge:Health Sciences - Pharmacy
Principal Investigator:Flavio da Silva Emery
Grantee:Júlia Possamai Gimenes
Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil


Aripiprazole fits in a new class of antipsychotic agents known as dopamine systems stabilizers (DSSs) that represent Dopamine D2 receptor partial agonists. Considering the already established shape and pharmacophore similarity the heterocyclic core present in the aripiprazole, dihydroquinolinone, and the heteroaromatic naphthyridone, the bioisosteric replacement of those structures is an alternative to obtainment of potentially psychoactive compounds. Thus, the present proposal aims the planning of a library of candidate compounds to antipsychotics derivatives of aripiprazole structure, as well as validation of the similarity between the structures, related derivatives and the parent molecule from psychoactive properties, observed by biological assays and experimental physicochemical properties.

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