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Last Updated: 07/11/2024

Asymmetric aminocatalysis in the synthesis of new artemisinin analogs

Objectives

*Original in Portuguese: Aminocatálise Assimétrica na Síntese de Novos Análogos de Artemisinina

This project proposes the synthetic preparation of a chemo-library of artemisinin analogues to assess their effectiveness against malaria, with a particular focus on resistant strains.

Principal Investigators / Focal Persons

Bruno Matos Paz

Rationale and Abstract

The potential application in tumor cells will also be studied with the main focus on verifying if there is cell death by ferroptosis. These syntheses will be guided by two main scopes: a pathway to Michael’s adducts obtaining analogues with differences in lacton ring connectivity and, mainly, containing the ozonide group as a possible pharmacophore group; the other via cycloaddition of silyl-ketene-bis-vinylic acetals in order to obtain analogues with the common artemisinin connections. Both scopes will have organocatalyzed steps to study enantioselectivity and perform studies of linear free energy relationships.

Thematic Categories

Drug-based Strategies

Date

Jun 2024 — Feb 2028

Project Site

Brazil

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