Primaquine-thiazolidinones block malaria transmission and development of the liver exoerythrocytic forms

Malaria Journal
Anna Caroline Campos AguiarA U Krettli


Primaquine is an anti-malarial used to prevent Plasmodium vivax relapses and malaria transmission. However, PQ metabolites cause haemolysis in patients deficient in the enzyme glucose-6-phosphate dehydrogenase (G6PD). Fifteen PQ-thiazolidinone derivatives, synthesized through one-post reactions from primaquine, arenealdehydes and mercaptoacetic acid, were evaluated in parallel in several biological assays, including ability to block malaria transmission to mosquitoes. All primaquine derivatives (PQ-TZs) exhibited lower cell toxicity than primaquine; none caused haemolysis to normal or G6PD-deficient human erythrocytes in vitro. Sera from mice pretreated with the test compounds thus assumed to have drug metabolites, caused no in vitro haemolysis of human erythrocytes, whereas sera from mice pretreated with primaquine did cause haemolysis. The ability of the PQ-TZs to block malaria transmission was evaluated based on the oocyst production and percentage of mosquitoes infected after a blood meal in drug pre-treated animals with experimental malaria caused by either Plasmodium gallinaceum or Plasmodium berghei; four and five PQ-TZs significantly inhibited sporogony in avian and in rodent malaria, respectively. Selected PQ-TZs were ...Continue Reading


Apr 1, 1988·Journal of Medicinal Chemistry·A PhilipF I Carroll
Jul 1, 1987·Journal of Medicinal Chemistry·E H ChenE A Nodiff
Dec 1, 1983·Archives of Toxicology·D Lorke
Apr 1, 1984·British Journal of Clinical Pharmacology·G W MihalyA M Breckenridge
Apr 1, 1983·Experimental Parasitology·R W GwadzD E Davidson
May 22, 2002·Journal of Ethnopharmacology·Maria do Céu de MadureiraVirgílio do Rosário
Sep 19, 2003·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·C BézivinJ Boustie
Oct 7, 2003·Bioorganic & Medicinal Chemistry·Suryanarayana VangapanduRahul Jain
Apr 1, 2004·Chemistry : a European Journal·Odile Dechy-CabaretBernard Meunier
May 6, 2004·Bioorganic & Medicinal Chemistry Letters·Sergio RomeoEnrica Bosisio
Sep 21, 2004·The Journal of Infectious Diseases·Douglas S WalshThomas G Brewer
Oct 21, 2004·Clinical Infectious Diseases : an Official Publication of the Infectious Diseases Society of America·J Kevin Baird, Stephen L Hoffman
Feb 4, 2005·Journal of Medicinal Chemistry·Maria João AraújoNuno Vale
Dec 8, 2006·Journal of Medicinal Chemistry·Mario Dell'AgliSergio Romeo
Jan 19, 2007·Journal of Medicinal Chemistry·V Raja SolomonS B Katti
Jun 10, 2008·Bioorganic & Medicinal Chemistry Letters·Nuno ValePaula Gomes
Oct 22, 2008·European Journal of Medicinal Chemistry·Nuno ValePaula Gomes
Nov 3, 2010·Biochemical and Biophysical Research Communications·Cui WangChengming Zeng
Sep 20, 2012·Methods in Molecular Biology·Photini SinnisMaria M Mota
May 7, 2013·European Journal of Medicinal Chemistry·Alice KunzlerWilson Cunico
Dec 21, 2013·European Journal of Medicinal Chemistry·Avinash C TripathiShailendra K Saraf
Jan 1, 2014·British Journal of Haematology·Lucio Luzzatto, Elisa Seneca
Jan 30, 2014·Proceedings of the National Academy of Sciences of the United States of America·Joel Vega-RodríguezMarcelo Jacobs-Lorena
Aug 17, 2016·Drug Design, Development and Therapy·Yehenew A EbstieDawit A Ejigu

❮ Previous
Next ❯


Feb 20, 2020·Biochemistry·Kuan-Yi Lu, Emily R Derbyshire

❮ Previous
Next ❯

Methods Mentioned

light microscopy
serum collection

Software Mentioned


Related Concepts

Related Feeds

Antimalarial Agents

Antimalarial agents, also known as antimalarials, are designed to prevent or cure malaria. Discover the latest research on antimalarial agents here.

Antimalarial Agents (ASM)

Antimalarial agents, also known as antimalarials, are designed to prevent or cure malaria. Discover the latest research on antimalarial agents here.