• Corpus ID: 37411754

Microsoft Word - 50

  title={Microsoft Word - 50},
  author={Sandeep Kumar Singh and Shailja Singh},
Development of new and more powerful antimalarial drugs has become more complex because of emergence of multidrug resistant strains of P. falciparum. Due to resistance of malaria parasite against well-known available drugs, the chemotherapy of malaria has become more complex and challenging. In this review we have discussed the life cycle of malaria parasite followed by quinoline based antimalarial drugs. Quinoline containing antimalarial compounds is the most effective class of drugs known for… 


Chemotherapy and drug resistance in malaria.
Recent work has identified the mechanism of resistance to the dihydrofolate reductase (DHFR) inhibitors as being due to point mutations within the DHFR gene that render the enzyme less susceptible to inhibition by the drugs.
Antimalarial drug discovery: old and new approaches
  • P. Rosenthal
  • Biology, Medicine
    Journal of Experimental Biology
  • 2003
A number of new antimalarial therapies will likely be needed over the coming years, so it is important to pursue multiple strategies for drug discovery.
Combination therapy for malaria: the way forward?
In large field trials, the combination of an artemisinin derivative and a partner drug with an unrelated mode of action (in this case mefloquine), has shown a remarkable double effect: preventing the emergence and spread of drug resistance, and interrupting the transmission of P. falciparum.
Discovery of dual function acridones as a new antimalarial chemotype
This innovative acridone design merges intrinsic potency and resistance-counteracting functions in one molecule, and represents a new strategy to expand, enhance and sustain effective antimalarial drug combinations.
Antimalarial drug resistance.
  • N. White
  • Biology, Medicine
    The Journal of clinical investigation
  • 2004
Widespread use of these drugs could roll back malaria and Artemisinin-derivative combinations are particularly effective, since they act rapidly and are well tolerated and highly effective.
Quinoline antimalarials: mechanisms of action and resistance and prospects for new agents.
As the malaria parasites become increasingly resistant to the quinoline antimalarials, there is an urgent need to understand the molecular mechanisms for drug action and resistance so that novel antimalarial drugs can be designed.
Strategies for the prevention of antimalarial drug resistance: rationale for combination chemotherapy for malaria.
In this review, Nick White and Piero Olliaro discuss the rationale for combination chemotherapy and the emergence and spread of parasite resistance to commonly used antimalarial drugs.
Quinoline antimalarials: mechanisms of action and resistance.
It is speculated that the quinolinemethanols bind to high density lipoproteins in the serum and are delivered to the erythrocytes where they interact with an ERYthrocyte membrane protein, known as stomatin, and are transferred to the intracellular parasite via a pathway used for the uptake of exogenous phospholipid.
Molecular basis of differential resistance to cycloguanil and pyrimethamine in Plasmodium falciparum malaria.
Analysis of the P. falciparum dihydrofolate reductase (DHFR) from different parasites reveals the structural basis for differential susceptibility to these antifolate drugs and suggests fine differences in binding within the active site cavity of DHFR.
Mefloquine (WR 142,490) in the treatment of human malaria
The marked activity of a single dose of mefloquine against chloroquine-resistant strains of Plasmodium falciparum suggests that this agent may be more useful than currently available drugs are for the treatment of drug-resistant malaria.