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Design, synthesis, and structure-activity relationship studies of 4-quinolinyl- and 9-acrydinylhydrazones as potent antimalarial agents. 2008
Caterina Fattorusso, and
Giuseppe Campiani, and
Gagan Kukreja, and
Marco Persico, and
Stefania Butini, and
Maria Pia Romano, and
Maria Altarelli, and
Sindu Ros, and
Margherita Brindisi, and
Luisa Savini, and
Ettore Novellino, and
Vito Nacci, and
Ernesto Fattorusso, and
Silvia Parapini, and
Nicoletta Basilico, and
Donatella Taramelli, and
Vanessa Yardley, and
Simon Croft, and
Marianna Borriello, and
Sandra Gemma
campiani@unisi.it.
Malaria is a major health problem in poverty-stricken regions where new antiparasitic drugs are urgently required at an affordable price. We report herein the design, synthesis, and biological investigation of novel antimalarial agents with low potential to develop resistance and structurally based on a highly conjugated scaffold. Starting from a new hit, the designed modifications were performed hypothesizing a specific interaction with free heme and generation of radical intermediates. This approach provided antimalarials with improved potency against chloroquine-resistant plasmodia over known drugs. A number of structure-activity relationship (SAR) trends were identified and among the analogues synthesized, the pyrrolidinylmethylarylidene and the imidazole derivatives 5r, 5t, and 8b were found as the most potent antimalarial agents of the new series. The mechanism of action of the novel compounds was investigated and their in vivo activity was assessed.
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