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

• Grant number: 18/01240-9
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: July 01, 2018
• End date: 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

Abstract

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 have been used in prodrug design. Based on foregoing information and taking into account that 3-hydroxyflavone showed to be leishmanicide 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 hexanediamine used as core wiil be used as carriers. The compounds will be synthesized and structurally characterized.