title: 4-aminoquinoline-triazine-based hybrids with improved in vitro antimalarial activity against CQ-sensitive and CQ-resistant strains of Plasmodium falciparum.
abstract: A systematic chemical modification in the triazine moiety covalently attached via suitable linkers to 4-amino-7-chloroquinolines yielded a series of new 7-chloro-4-aminoquinoline-triazine hybrids exhibiting high in vitro activity against W2 (chloroquine-resistant) and D6 (chloroquine-sensitive) strains of Plasmodium falciparum without any toxicity against mammalian cell lines (Vero, LLC-PK11, HepG2). Many of the compounds (6, 8, 10, 11, 13, 14, 16, 27, 29 and 33) showed excellent potency against chloroquine sensitive and resistant strains. In particular, compounds 6, 8, 14, 16 and 29 were found to be significantly more active than chloroquine against the chloroquine-resistant strains (W2 clone) of P. falciparum.
authors: Department of Chemistry, University of Delhi, Delhi, India.
authors: Sunny
authors: S
authors: Manohar
authors: Shabana I
authors: SI
authors: Khan
authors: Diwan S
authors: DS
authors: Rawat
mesh_terms: D000634:Aminoquinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002522:Chlorocebus aethiops; D002738:Chloroquine / Q000737:chemistry / Q000494:pharmacology; D004351:Drug Resistance / Q000187:drug effects*; D056945:Hep G2 Cells; D006801:Humans; D016778:Malaria, Falciparum / Q000188:drug therapy / Q000378:metabolism; D010963:Plasmodium falciparum / Q000378:metabolism*; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D014709:Vero Cells
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; D014227:Triazines; D002738:Chloroquine; C001920:4-aminoquinoline