Potential leishmanicides: synthesis of first generation hydroxymethylnitrofural drug targeted dendrimers

• Grant number: 10/03651-4
• Support Opportunities: Scholarships in Brazil - Master
• Start date: August 01, 2010
• End date: July 31, 2012
• Field of knowledge: Health Sciences - Pharmacy
• Principal Investigator: Elizabeth Igne Ferreira
• Grantee: Soraya da Silva Santos
• Host Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

Due to the urgent need of leishmanicides, this project comprehends the synthesis of first generation dendrimer targeted drugs of hydroxymethylnitrofural (NFOH), that showed potential leishmanicide activity, as observed by our research group (unpublished data). With this goal, we intend to develop NFOH targeted drugs with selective action in macrophages, due to the presence of mannose in the structure, and also NFOH targeted drugs that present selectivity for the parasite, due to the presence of inositol in the structure. The dendrimers will have inositol (core group) and dendrons built with the promising compound - NFOH. To the external groups of dendrimers, mannose and inositol which are responsible for directing the compound to the site of action, respectively, macrophage and into the parasite, will be linked. Molecular modeling will be used to support the studies about compound release from the targeted drugs synthesized. The mechanism of releasing can comprehend either hydrolysis of the esters directly linked to inositol, with further hydrolysis of NFOH and of the maleil carrier, or initial hydrolyses of the external branches, until inositol in the dendrimer core has been released. (AU)

Academic Publications

(References retrieved automatically from State of São Paulo Research Institutions)

SANTOS, Soraya da Silva. Potencial leishmanicides: synthesis study of first generation dendrimer targeted drugs with hydroxymethylnitrofurazone. 2012. Master's Dissertation - Universidade de São Paulo (USP). Conjunto das Químicas (IQ e FCF) (CQ/DBDCQ) São Paulo.