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Full-Text Articles in Microbiology
The Plasmodium Falciparum Chloroquine Resistance Transporter, Pfcrt, Mediates The Activity Of Chloroquine-Resistance Reversal Agents In The Malaria Parasite, Kristin Lane
Biological Sciences Theses & Dissertations
Chloroquine (CQ) resistant Plasmodium falciparum is a serious problem affecting 3.2 billion people in over 100 countries today. Most endemic malarious countries are among the poorest in the world and lack the resources to replace the inexpensive and highly effective CQ. CQ resistance (CQR) reversal agents are a potentially inexpensive solution to restoring CQ efficacy. CQR reversal agents are drugs that have little to no antimalarial activity alone, but in combination with CQ, they increase dmg accumulation in the parasite and enhance the sensitivity to CQ in CQR parasites. PfCRT is a putative transporter located on the parasite digestive vacuole …
Design, Synthesis, And Evaluation Of 10-N-Substituted Acridones As Novel Chemosensitizers In Plasmodium Falciparum, Jane X. Kelly, Martin J. Smilkstein, Roland A. Cooper, Kristin D. Lane, Robert A. Johnson, Aaron Janowsky, Rozalia A. Dodean, David J. Hinrichs, Rolf Winter, Michael Riscoe
Design, Synthesis, And Evaluation Of 10-N-Substituted Acridones As Novel Chemosensitizers In Plasmodium Falciparum, Jane X. Kelly, Martin J. Smilkstein, Roland A. Cooper, Kristin D. Lane, Robert A. Johnson, Aaron Janowsky, Rozalia A. Dodean, David J. Hinrichs, Rolf Winter, Michael Riscoe
Biological Sciences Faculty Publications
A series of novel 10-N-substituted acridones, bearing alkyl side chains with tertiary amine groups at the terminal position, were designed, synthesized, and evaluated for the ability to enhance the potency of quinoline drugs against multidrug-resistant (MDR) Plasmodium falciparum malaria parasites. A number of acridone derivatives, with side chains bridged three or more carbon atoms apart between the ring nitrogen and terminal nitrogen, demonstrated chloroquine (CQ)-chemosensitizing activity against the MDR strain of P. falciparum (Dd2). Isobolograrn analysis revealed that selected candidates demonstrated significant synergy with CQ in the CQ-resistant (CQR) parasite Dd2 but only additive (or indifferent) interaction in the CQ-sensitive …