Whole-cell SYBR Green I assay for antimalarial activity assessment

Authors: Lobo E, Machado M, Murtinheira F, Nogueira F
Publication Year: 2016
Journal: Annals of Clinical and Medical Microbiology
Link: https://www.jscimedcentral.com/MedicalMicrobiology/earlyonline.php%20

Malaria parasite growth assessment assays using nucleic acid dye SYBR GreenI are frequently compromised by high background readings due to haemoglobin and detergents in lysis buffer. Here, we have assessed and further validated an intact-cell SYBR Green I-based fluorescence assay (Cell-MSF) for antimalarial activity assessment even of highly fluorescent compounds. Our modifications include:
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Primaquine-based ionic liquids as a novel class of antimalarial hits

Authors: D'Alessandro S, Ferraz R, Gomes A, Gomes P, Machado M, Murtinheira F, Nogueira F, Noronha J, Parapini S, Prudêncio C, Prudencio M, Teixeira C
Publication Year: 2016
Journal: RCS Advances
Link: http://pubs.rsc.org/en/Content/ArticleLanding/2016/RA/C6RA10759A#!divAbstract%20

Ionic liquids derived from active pharmaceutical ingredients may open new perspectives towards low-cost rescuing of classical drugs. Thus, we have synthesized novel ionic liquids derived from the antimalarial drug primaquine, and evaluated them in vitro against three stages of malaria parasites. Results from this unprecedented approach open a new chapter in the history of antimalarial […]
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On the ordeal of quinolone preparation via cyclisation of aryl-enamines; Synthesis and structure of ethyl 6-methyl-7-iodo-4-(3-iodo-4-methylphenoxy)-quinoline-3-carboxylate

Authors: Brás EM, Cristiano MLS, Fausto R, Henriques MSC, Horta P, Murtinheira F, Nogueira F, O'Neill PM, Paixão JA
Publication Year: 2017
Journal: Pure and Applied Chemistry
Link: https://www.degruyter.com/view/j/pac.2017.89.issue-6/pac-2016-1119/pac-2016-1119.xml

Recent studies directed to the design of compounds targeting the bc1 protein complex of Plasmodium falciparum, the parasite responsible for most lethal cases of malaria, identified quinolones (4-oxo-quinolines) with low nanomolar inhibitory activity against both the enzyme and infected erythrocytes. The 4-oxo-quinoline 3-ester chemotype emerged as a possible source of potent bc1 inhibitors, prompting us to expand the library of available […]
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Synthesis and antimalarial evaluation of prodrugs of novel fosmidomycin analogues

Authors: Barros MT, Faisca Phillips AM, Murtinheira F, Nogueira F
Publication Year: 2015
Journal: Bioorganic & Medicinal Chemistry Letters
Link: http://www.ncbi.nlm.nih.gov/pubmed/25881827

The continuous development of drug resistance by Plasmodium falciparum, the agent responsible for the most severe forms of malaria, creates the need for the development of novel drugs to fight this disease.
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Whole-cell SYBR Green I assay for antimalarial activity assessment

Primaquine-based ionic liquids as a novel class of antimalarial hits

On the ordeal of quinolone preparation via cyclisation of aryl-enamines; Synthesis and structure of ethyl 6-methyl-7-iodo-4-(3-iodo-4-methylphenoxy)-quinoline-3-carboxylate

Synthesis and antimalarial evaluation of prodrugs of novel fosmidomycin analogues

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