title: Synthesis and in vitro evaluation of new chloroquine-chalcone hybrids against chloroquine-resistant strain of Plasmodium falciparum.
abstract: The control of malaria has been complicated with increasing resistance of malarial parasite against existing antimalarials. Herein, we report the synthesis of a new series of chloroquine-chalcone based hybrids (8-22) and their antimalarial efficacy against both chloroquine-susceptible (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum. Most of the compounds showed enhanced antimalarial activity as compared to chloroquine in chloroquine-resistant (K1) strain of Plasmodium falciparum. Furthermore, to unfold the mechanism of action of these synthesized hybrid molecules, we carried out hemin dependent studies, in which three compounds were found to be active.
authors: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226 001, India. kv_sashidhara@cdri.res.in
authors: Koneni V
authors: KV
authors: Sashidhara
authors: Srinivasa Rao
authors: SR
authors: Avula
authors: Gopala Reddy
authors: GR
authors: Palnati
authors: Shiv Vardan
authors: SV
authors: Singh
authors: Kumkum
authors: K
authors: Srivastava
authors: Sunil K
authors: SK
authors: Puri
authors: J K
authors: JK
authors: Saxena
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D002599:Chalcone / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D002738:Chloroquine / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004351:Drug Resistance; D006427:Hemin / Q000378:metabolism; D006801:Humans; D016778:Malaria, Falciparum / Q000188:drug therapy; D010963:Plasmodium falciparum / Q000187:drug effects*; D014709:Vero Cells
chemical_list: D000962:Antimalarials; D002599:Chalcone; D006427:Hemin; D002738:Chloroquine