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Studies concerning the effect of a methylene spacer group in marinoquinolines: synthesis and biological evaluation

Grant number: 19/04803-7
Support type:Scholarships in Brazil - Scientific Initiation
Effective date (Start): April 01, 2019
Effective date (End): March 31, 2020
Field of knowledge:Physical Sciences and Mathematics - Chemistry
Principal Investigator:Carlos Roque Duarte Correia
Grantee:Ítalo Caetano Canevari da Silva
Home Institution: Instituto de Química (IQ). Universidade Estadual de Campinas (UNICAMP). Campinas , SP, Brazil
Associated research grant:14/25770-6 - New frontiers in cross-coupling reactions promoted by palladium: combining enantioselective catalysis, C-H activations, new materials and in flux reactions aiming at high efficiency and sustainability in synthetic processes, AP.TEM

Abstract

Marinoquinolines are a new class of quinoline compounds, which were discovered in marine bacteria, presenting good antimalarial activity. Currently there are several synthetic routes for its preparation, however, the synthetic route employed by our research group allowed the development of a marinoquinoline libraries. Continuing the study of this class of compounds, in collaboration with the research group of Prof. Dr. Rafael Guido, from USP - São Carlos, we found the lead compound MQ-30 (IC50 39 nM and SI > 6400). Despite its promising activity, MQ-30 presents moderate in vivo activity. Moreover, there is the need to improve its physicochemical properties, such as solubility and LogP. Therefore, this project aims at obtaining new derivatives of MQ-30, as well as other antimalarial compounds incorporating a flexible tether in the form of a methylene-type spacer group. These new molecules will be subjected to biological tests in order to find new promising lead-compounds for the treatment of malaria.