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4‐Aminoquinoline‐Triazine‐Based Hybrids with Improved In Vitro Antimalarial Activity Against CQ ‐Sensitive and CQ ‐Resistant Strains of P lasmodium falciparum
Author(s) -
Manohar Sunny,
Khan Shabana I.,
Rawat Diwan S.
Publication year - 2013
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12108
Subject(s) - chloroquine , plasmodium falciparum , in vitro , moiety , chemistry , potency , triazine , clone (java method) , pharmacology , stereochemistry , biochemistry , biology , malaria , dna , immunology , organic chemistry
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 W 2 (chloroquine‐resistant) and D 6 (chloroquine‐sensitive) strains of P lasmodium falciparum without any toxicity against mammalian cell lines ( V ero, LLC ‐ PK 11, H ep G 2). 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 ( W 2 clone) of P . falciparum .