Synthesis of novel thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials.
In search of new 4-aminoquinolines which are not recognized by CQR mechanism, thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline were synthesized and screened for their antimalarial activities. Thiourea derivative 3 found to be the most active against CQ sensitive strain 3D7 of Plasmodium falciparum in an in vitro model with an IC(50) of 6.07ng/mL and also showed an in vivo suppression of 99.27% on day 4 against CQ resistant strain N-67 of Plasmodium yoelii.
Sunduru
Naresh
N
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226 001, India.
Srivastava
Kumkum
K
Rajakumar
S
S
Puri
S K
SK
Saxena
J K
JK
Chauhan
Prem M S
PM