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Synthesis of the first generation dendrimer prodrugs of 3-hydroxyflavone potentially leishmanicides

Grant number: 18/01240-9
Support Opportunities:Scholarships in Brazil - Scientific Initiation
Effective date (Start): July 01, 2018
Effective date (End): June 30, 2019
Field of knowledge:Health Sciences - Pharmacy
Principal Investigator:Elizabeth Igne Ferreira
Grantee:Cinthya Miyuki Sano
Host Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil


Leishmaniasis is a neglected disease of high incidence in many countries, including Brazil. There are few effective chemotherapeutic agents against this disease, therefore, is urgent the search for better therapeutic agents. On the other hand, prodrug design is a molecular modification process that, by means of carriers, allows the improvement of drug or bioactive compounds activity. Concerning the carriers, dendrimers, a polymer class of many structural architectures has been used in prodrug design. Based on foregoing information and taking into account that 3-hydroxy flavone showed to be leishmanicidal in vitro with low in vivo bioavailability, the purpose of this work is to synthesize dendrimer prodrugs of this compound, with the aim of improving its activity. Dendrimer derived of Bis-MPA with butane- and hexane diamine used as core will be used as carriers. The compounds will be synthesized and structurally characterized.

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