title: Synthesis of novel thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials.
abstract: 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.
authors.affiliation: Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226 001, India.
authors.forename: Naresh
authors.initials: N
authors.lastname: Sunduru
authors.forename: Kumkum
authors.initials: K
authors.lastname: Srivastava
authors.forename: S
authors.initials: S
authors.lastname: Rajakumar
authors.forename: S K
authors.initials: SK
authors.lastname: Puri
authors.forename: J K
authors.initials: JK
authors.lastname: Saxena
authors.forename: Prem M S
authors.initials: PM
authors.lastname: Chauhan