title: Design and synthesis of new antimalarial agents from 4-aminoquinoline.
abstract: This study describes the synthesis of new 4-aminoquinoline derivatives and evaluation of their activity against a chloroquine sensitive strain of P. falciparum in vitro and chloroquine resistant N-67 strain of P. yoelii in vivo. All the analogues were found to form strong complex with hematin and inhibit the beta-hematin formation in vitro. These results suggest that these compounds act on heme polymerization target.
authors.affiliation: Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226 001, India.
authors.forename: V Raja
authors.initials: VR
authors.lastname: Solomon
authors.forename: Sunil K
authors.initials: SK
authors.lastname: Puri
authors.forename: Kumkum
authors.initials: K
authors.lastname: Srivastava
authors.forename: S B
authors.initials: SB
authors.lastname: Katti
mesh_terms: D000634:Aminoquinolines / Q000737:chemistry*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D002738:Chloroquine / Q000494:pharmacology; D015195:Drug Design; D004351:Drug Resistance; D006427:Hemin / Q000378:metabolism; D008288:Malaria / Q000188:drug therapy / Q000469:parasitology; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010967:Plasmodium yoelii / Q000187:drug effects / Q000502:physiology; D013329:Structure-Activity Relationship
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; D006427:Hemin; D002738:Chloroquine; C001920:4-aminoquinoline