204568-74-1Relevant articles and documents
NITROGEN-CONTAINING TRICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE
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Page/Page column 54; 55, (2018/03/01)
A nitrogen-containing tricyclic compound which acts as modulator of FXR, or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and the use of the compoun
Design, synthesis, and structure-activity relationship studies of 4-quinolinyl- and 9-acrydinylhydrazones as potent antimalarial agents
Fattorusso, Caterina,Campiani, Giuseppe,Kukreja, Gagan,Persico, Marco,Butini, Stefania,Romano, Maria Pia,Altarelli, Maria,Ros, Sindu,Brindisi, Margherita,Savini, Luisa,Novellino, Ettore,Nacci, Vito,Fattorusso, Ernesto,Parapini, Silvia,Basilico, Nicoletta,Taramelli, Donatella,Yardley, Vanessa,Croft, Simon,Borriello, Marianna,Gemma, Sandra
, p. 1333 - 1343 (2008/09/20)
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.
