Synthesis, characterization, and antimalarial activity of novel schiff-base-phenol and naphthalene-amine ligands.
Emergence of chloroquine (CQ) resistant Plasmodium falciparum strains necessitates discovery of inexpensive antimalarial drugs capable of targeting CQ-resistant strains. Towards this objective, herein we have synthesized and characterized naphthalene-Schiff bases or naphthalene-amine phenols. Among these compounds, 7 demonstrated a significant bioactivity with a half-maximal inhibitory concentration (IC(50)) of 1.7 microM against CQ-resistant Dd2 strains.
Harpstrite
Scott E
SE
Mallinckrodt Institute of Radiology, Washington University Medical School, St Louis, MO 63110, USA.
Collins
Silvia D
SD
Oksman
Ana
A
Goldberg
Daniel E
DE
Sharma
Vijay
V
D000588:Amines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008024:Ligands; D015394:Molecular Structure; D009281:Naphthalenes / Q000737:chemistry*; D019800:Phenol / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects; D012545:Schiff Bases / Q000737:chemistry
D000588:Amines; D000962:Antimalarials; D008024:Ligands; D009281:Naphthalenes; D012545:Schiff Bases; C031721:naphthalene; D019800:Phenol