Piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates: Synthesis and antiplasmodial evaluation.
A series of piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates were prepared with a view to evaluate their activities against Plasmodium falciparum. The synthesized conjugates had in vitro IC50values from 0.41 to 2.38 μm against chloroquine-resistant and mefloquine-sensitive W2 strain of P. falciparum. The submicromolar activities of most of the synthesized conjugates suggest that such molecular frameworks can act as therapeutic templates for the design and synthesis of new antimalarials.
Department of Chemistry, Guru Nanak Dev University, Amritsar, Punjab, India.
Amandeep
A
Singh
Department of Chemistry, Guru Nanak Dev University, Amritsar, Punjab, India.
Anu
A
Rani
Department of Medicine, University of California, San Francisco, CA, USA.
Jiri
J
Gut
Department of Medicine, University of California, San Francisco, CA, USA.
Philip J
PJ
Rosenthal
Department of Chemistry, Guru Nanak Dev University, Amritsar, Punjab, India.
Vipan
http://orcid.org/0000-0002-6164-7161
V
Kumar
D000634:Aminoquinolines / Q000737:chemistry* / Q000494:pharmacology*; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology*; D002599:Chalcone / Q000737:chemistry / Q000494:pharmacology; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance; D005296:Ferrous Compounds / Q000737:chemistry / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D016778:Malaria, Falciparum / Q000188:drug therapy; D010879:Piperazines / Q000737:chemistry* / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects*
D000634:Aminoquinolines; D000962:Antimalarials; D005296:Ferrous Compounds; D010879:Piperazines; D002599:Chalcone; D002738:Chloroquine; C001920:4-aminoquinoline
4-aminoquinoline-ferrocenyl-chalcone; aldol condensation; antiplasmodial activities; structure-activity relationship