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

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

Abstract

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.