Synthesis, antimalarial activity and cytotoxicity of 4-aminoquinoline-triazine conjugates.
A series of 4-aminoquinoline-triazine conjugates with different substitution pattern have been synthesized and evaluated for their in vitro antimalarial activity against chloroquine-sensitive and resistant strains of Plasmodium falciparum. Compounds 16, 19, 28 and 35 exhibited promising antimalarial activity against both strains of P. falciparum. Cytotoxicity of these compounds was tested against three cell lines. Several compounds did not show any cytotoxicity up to a high concentration (48microM), others exhibited mild toxicities but selective index for antimalarial activity was high for most of these conjugates.
Manohar
Sunny
S
Department of Chemistry, University of Delhi, Delhi 110 007, India.
Khan
Shabana I
SI
Rawat
Diwan S
DS
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D002522:Chlorocebus aethiops; D002738:Chloroquine / Q000737:chemistry; D056945:Hep G2 Cells; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects; D014227:Triazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D014709:Vero Cells
D000634:Aminoquinolines; D000962:Antimalarials; D014227:Triazines; D002738:Chloroquine; C001920:4-aminoquinoline