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Design, synthesis and in vitro antiplasmodial activity of some bisquinolines against chloroquine‐resistant strain
Author(s) -
Kondaparla Srinivasarao,
Agarwal Pooja,
Srivastava Kumkum,
Puri Sunil K.,
Katti Seturam B.
Publication year - 2017
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.12914
Subject(s) - chloroquine , plasmodium falciparum , ic50 , in vitro , strain (injury) , antimalarial agent , chemistry , amine gas treating , stereochemistry , pharmacology , biology , malaria , biochemistry , organic chemistry , immunology , anatomy
A series of novel bisquinoline compounds comprising N 1 ‐(7‐chloroquinolin‐4‐yl) ethane‐1,2‐diamine and 7‐chloro‐ N ‐(2‐(piperazin‐1‐yl)ethyl)quinolin‐4‐amine connected with 7‐chloro‐4‐aminoquinoline containing various amino acids is described. We have bio‐evaluated the compounds against both chloroquine‐sensitive (3D7) and chloroquine‐resistant (K1) strains of Plasmodium falciparum in vitro. Among the series, compounds 4 and 7 exhibited 1.8‐ and 10.6‐fold superior activity as compared to chloroquine (CQ; IC 50 = 0.255 ± 0.049 μ m ) against the K1 strain with IC 50 values 0.137 ± 0.014 and 0.026 ± 0.007 μ m , respectively. Furthermore, compound 7 also displayed promising activity against the 3D7 strain (IC 50 = 0.024 ± 0.003 μ m ) of P. falciparum when compared to CQ. All the compounds in the series displayed resistance factor between 0.57 and 4.71 as against 51 for CQ. These results suggest that bisquinolines can be explored for further development as new antimalarial agents active against chloroquine‐resistant P. falciparum .