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DEVELOPMENT OF NEW MARINOQUINOLINES AS ANTIMALARIAL AGENTS: DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION

Grant number: 18/03143-0
Support type:Scholarships in Brazil - Doctorate
Effective date (Start): October 01, 2018
Status:Discontinued
Field of knowledge:Physical Sciences and Mathematics - Chemistry - Organic Chemistry
Principal Investigator:Carlos Roque Duarte Correia
Grantee:Patricia Santos Barbosa
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

Marinoquinoline is a class of quinoline derivatives originally found in marine bacteria. Currently, there are several synthetic routes to obtain the marinoquinoline nucleus, which has already allowed the synthesis of several synthetic analogues. Due to its structural similarity with quinolines, our research group synthesized a series of unpublished marinoquinolines and evaluated their biological activity in Plasmodium falciparum 3d7 strains, in partnership with the research group of Prof. Dr. Rafael Guido, from USP - São Carlos. The main result of this initial study was a lead compound, encoded as MQ-030, with high potency and selectivity. Faced with this result, there is now a need for optimizations of both power and physicochemical properties. For this, we count on the help of the research group of Prof. Dr. Rafael Guido, with the prior development of a QSAR model and biological evaluations. Thus, our function is the synthesis of new marinoquinolines, containing the necessary structural changes to rationally improve potency.