Synthesis and Effects on Chloroquine Susceptibility in Plasmodium falciparum of a Series of New Dihydroanthracene Derivatives
- 20 June 2002
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 45 (15) , 3195-3209
- https://doi.org/10.1021/jm011046l
Abstract
To suggest a mechanism of action for drugs capable to reverse the chloroquine resistance, a new set of 9,10-dihydro-9,10-ethano and ethenoanthracene derivatives was synthesized and compounds were tested with the aim to assess their effect on chloroquine susceptibility in Plasmodium falciparum resistant strains. With respect to this, reversal of resistance and change in drug accumulation were compared. Structure−activity relationship and molecular modeling studies made it possible to define a pharmacophoric moiety for reversal agents and to propose a putative model of interaction with some selected amino acids.Keywords
This publication has 23 references indexed in Scilit:
- Analysis of pfcrt point mutations and chloroquine susceptibility in isolates of Plasmodium falciparumMolecular and Biochemical Parasitology, 2001
- Heteroaryl Analogues of AMPA. Synthesis and Quantitative Structure−Activity RelationshipsJournal of Medicinal Chemistry, 1997
- A P-glycoprotein homologue of Plasmodium falciparum is localized on the digestive vacuole.The Journal of cell biology, 1991
- Amplification of the multidrug resistance gene in some chloroquine-resistant isolates of P. falciparumCell, 1989
- Reversal of Chloroquine Resistance in Malaria Parasite Plasmodium falciparum by DesipramineScience, 1988
- Studies on the molybdenum cofactor: model synthetic routes directed at Form BThe Journal of Organic Chemistry, 1988
- Free-radical participation in the reactions of selected metalate anions with alkyl halidesJournal of the American Chemical Society, 1978
- Cyanohydridoborate anion as a selective reducing agentJournal of the American Chemical Society, 1971
- Catalytic dimerization of ethylene and propylene by nitrogentris(triphenylphosphine)cobalt hydrideJournal of the American Chemical Society, 1968
- High-Boiling Hydrolytic Derivatives of LigninJournal of the American Chemical Society, 1947