Application of organometallic reagents in the synthesis of new quinoline derivatives with potential antimalarial activity

• Grant number: 13/00758-0
• Support Opportunities: Scholarships in Brazil - Master
• Start date: September 01, 2013
• End date: January 31, 2015
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Giuliano Cesar Clososki
• Grantee: Paula Valim Nicolino
• Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil

Abstract

Although malaria is currently among the diseases with the greatest impact causing the death of 1 to 3 million people each year in developing countries, the development of new antimalarial drugs has been neglected since the 1970s. The therapy has a limited number of drugs available for the treatment of this pathology, among which stand out the quinoline compounds functionalized derivatives. Modern organometallic reagents such as i-PrMgCl.LiCl and the recently developed mixed lithium magnesium amides, have been successfully applied in the functionalization of aromatic and heterocyclic compounds. However, its reactivity with important substrates such as quinolines, has not been studied properly. Thus, the main aim of this project is to apply new organometallic reagents in the preparation of new functionalized quinolines with potential antimalarial activity. The synthesis of a novel hybrid molecular planned with pharmacophoric groups of two drugs useful against malaria (chloroquine and pyrimethamine) is also proposed as well as the preparation of chloroquine analogues substituted with different functional groups.

Scientific publications

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

MURIE, VALTER E.; NICOLINO, V, PAULA; DOS SANTOS, THIAGO; GAMBACORTA, GUIDO; NISHIMURA, V, RODOLFO H.; PEROVANI, ICARO S.; FURTADO, LUCIANA C.; COSTA-LOTUFO, V, LETICIA; DE OLIVEIRA, ANDERSON MORAES; VESSECCHI, RICARDO; et al. Synthesis of 7-Chloroquinoline Derivatives Using Mixed Lithium-Magnesium Reagents. Journal of Organic Chemistry, v. 86, n. 19, p. 13402-13419, OCT 1 2021. (13/00758-0, 15/21364-6, 19/05838-9, 18/14150-8, 15/17177-6)

Academic Publications

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

NICOLINO, Paula Valim. Application of organometallic reagents in the synthesis of new quinoline derivatives of medicinal interest. 2015. Master's Dissertation - Universidade de São Paulo (USP). Faculdade de Ciências Farmacêuticas de Ribeirão Preto (PCARP/BC) Ribeirão Preto.