Design and synthesis of new antimalarial agents from 4-aminoquinoline.
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.
Solomon
V Raja
VR
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226 001, India.
Puri
Sunil K
SK
Srivastava
Kumkum
K
Katti
S B
SB
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
D000634:Aminoquinolines; D000962:Antimalarials; D006427:Hemin; D002738:Chloroquine; C001920:4-aminoquinoline