scholarly journals Modified Fixed-Ratio Isobologram Method for Studying In Vitro Interactions between Atovaquone and Proguanil or Dihydroartemisinin against Drug-Resistant Strains of Plasmodium falciparum

2004 ◽  
Vol 48 (11) ◽  
pp. 4097-4102 ◽  
Author(s):  
Quinton L. Fivelman ◽  
Ipemida S. Adagu ◽  
David C. Warhurst
Keyword(s):  
Plasmodium Falciparum ◽  
Treatment Failure ◽  
Resistant Strain ◽  
Fixed Ratio ◽  
Drug Resistant ◽  
Resistant Strains ◽  
Drug Resistant Strains ◽  
In Vitro Interactions

ABSTRACT A modified fixed-ratio isobologram method for studying the in vitro interactions between antiplasmodial drugs is described. This method was used to examine the interactions between atovaquone, proguanil, and dihydroartemisinin. The interaction between atovaquone and proguanil was synergistic against atovaquone-sensitive strains K1 and T996; however, there was a loss of synergy against atovaquone-resistant strain NGATV01 isolated after Malarone (the combination of atovaquone and proguanil) treatment failure. While the interaction between atovaquone and dihydroartemisinin was indifferent against isolate NGATV01, the interaction displayed indifference tending toward antagonism against the atovaquone-sensitive strains tested. The relevance of in vitro interactions to in vivo treatment is discussed.

scholarly journals In Vitro and In Vivo Antimalarial Activities of a Carbohydrate Antibiotic, Prumycin, against Drug-resistant Strains of Plasmodia

2004 ◽  
Vol 57 (6) ◽  
pp. 400-402 ◽  
Author(s):  
KAZUHIKO OTOGURO ◽  
AKI ISHIYAMA ◽  
MIYUKI KOBAYASHI ◽  
HITOMI SEKIGUCHI ◽  
TAKASHI IZUHARA ◽  
...  
Keyword(s):  
Drug Resistant ◽  
Resistant Strains ◽  
Drug Resistant Strains

scholarly journals Sontochin as a Guide to the Development of Drugs against Chloroquine-Resistant Malaria

2012 ◽  
Vol 56 (7) ◽  
pp. 3475-3480 ◽  
Author(s):  
Sovitj Pou ◽  
Rolf W. Winter ◽  
Aaron Nilsen ◽  
Jane Xu Kelly ◽  
Yuexin Li ◽  
...  
Keyword(s):  
Multidrug Resistant ◽  
Plasmodium Yoelii ◽  
Significant Activity ◽  
Drug Resistant ◽  
Content Type ◽  
Resistant Strains ◽  
Drug Resistant Strains ◽  
Derivatives Of

ABSTRACTSontochin was the original chloroquine replacement drug, arising from research by Hans Andersag 2 years after chloroquine (known as “resochin” at the time) had been shelved due to the mistaken perception that it was too toxic for human use. We were surprised to find that sontochin, i.e., 3-methyl-chloroquine, retains significant activity against chloroquine-resistant strains ofPlasmodium falciparum in vitro. We prepared derivatives of sontochin, “pharmachins,” with alkyl or aryl substituents at the 3 position and with alterations to the 4-position side chain to enhance activity against drug-resistant strains. Modified with an aryl substituent in the 3 position of the 7-chloro-quinoline ring, Pharmachin 203 (PH-203) exhibits low-nanomolar 50% inhibitory concentrations (IC50s) against drug-sensitive and multidrug-resistant strains andin vivoefficacy against patent infections ofPlasmodium yoeliiin mice that is superior to chloroquine. Our findings suggest that novel 3-position aryl pharmachin derivatives have the potential for use in treating drug resistant malaria.

Synthesis and antimalarial activity of new 4-aminoquinolines active against drug resistant strains

RSC Advances ◽  
2016 ◽  
Vol 6 (107) ◽  
pp. 105676-105689 ◽  
Author(s):  
Srinivasarao Kondaparla ◽  
Awakash Soni ◽  
Ashan Manhas ◽  
Kumkum Srivastava ◽  
Sunil K. Puri ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Drug Resistant ◽  
New Class ◽  
Resistant Strains ◽  
Drug Resistant Strains

In the present study we have synthesized a new class of 4-aminoquinoline derivatives and bioevaluated them for antimalarial activity against theP. falciparum in vitro(3D7 & K1) andP. yoelii in vivo(N-67 strain).

scholarly journals Multistage antiplasmodial activity of hydroxyethylamine compounds, in vitro and in vivo evaluations

RSC Advances ◽  
2020 ◽  
Vol 10 (58) ◽  
pp. 35516-35530
Author(s):  
Neha Sharma ◽  
Yash Gupta ◽  
Meenakshi Bansal ◽  
Snigdha Singh ◽  
Prateek Pathak ◽  
...  
Keyword(s):  
Human Population ◽  
Antiplasmodial Activity ◽  
Drug Resistant ◽  
Fast Growing ◽  
Resistant Strains ◽  
Global Threat ◽  
Drug Resistant Strains

Malaria, a global threat to the human population, remains a challenge partly due to the fast-growing drug-resistant strains of Plasmodium species.

scholarly journals In Vitro Efficacies, ADME, and Pharmacokinetic Properties of Phenoxazine Derivatives Active against Mycobacterium tuberculosis

2019 ◽  
Vol 63 (11) ◽  
Author(s):  
Lloyd Tanner ◽  
Joanna C. Evans ◽  
Ronnett Seldon ◽  
Audrey Jordaan ◽  
Digby F. Warner ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Infected Animal ◽  
Mechanisms Of Action ◽  
Drug Resistant ◽  
Content Type ◽  
Pharmacokinetic Properties ◽  
Resistant Strains ◽  
Drug Resistant Strains

ABSTRACT Mycobacterium tuberculosis, the causative agent of tuberculosis, remains a leading infectious killer globally, demanding the urgent development of faster-acting drugs with novel mechanisms of action. Riminophenazines such as clofazimine are clinically efficacious against both drug-susceptible and drug-resistant strains of M. tuberculosis. We determined the in vitro anti-M. tuberculosis activities, absorption, distribution, metabolism, and excretion properties, and in vivo mouse pharmacokinetics of a series of structurally related phenoxazines. One of these, PhX1, displayed promising drug-like properties and potent in vitro efficacy, supporting its further investigation in an M. tuberculosis-infected animal model.

Immunity in trypanosomiasis

Parasitology ◽  
1959 ◽  
Vol 49 (1-2) ◽  
pp. 143-152 ◽  
Author(s):  
M. A. Soltys
Keyword(s):  
Resistant Strain ◽  
Therapeutic Dose ◽  
Sensitive Strain ◽  
Drug Resistant ◽  
Chemotherapeutic Drugs ◽  
Natural Conditions ◽  
Resistant Strains ◽  
Drug Resistant Strains

Antibody-resistant strains are less sensitive to suramin and antrycide than antibody-sensitive strains. When living trypanosomes were exposed to suramin and antrycide in vitro, antibody-resistant strains needed 50 times more drugs than antibody-sensitive trypanosomes in order to make them non-infectious to mice. In therapeutic experiments in mice the minimal therapeutic dose of drugs for antibody-sensitive strains was 0·1 mg. but for resistant strains it was 0·3 mg./20 g. mice. Rabbits treated prophylactically with suramin resisted infection with the antibody-sensitive strain for a period of 4 months, but failed to resist infection with the antibody-resistant strain after 2 months.Rabbits treated prophylactically with antrycide pro-salt, resisted infection with antibody-sensitive strains for a period of 2 months, but failed to resist infection with the antibody-resistant strain even 1 month after injection with the drug. Although trypanosomes can become drug resistant without being antibody resistant it is suggested that, under natural conditions, drug-resistant strains in animals and man develop from antibody-resistant strains, particularly when trypanostatic drugs are used. It is suggested in conclusion from these experiments that strains of trypanosomes which are exposed for some time to antibodies and become antibody resistant after passage through animals like rabbits, as well as those strains frequently passaged through mice, should be used in all tests for the efficiency of chemotherapeutic drugs.

scholarly journals In Vitro and in Vivo Antimalarial Activities of a Non-glycosidic 18-Membered Macrolide Antibiotic, Borrelidin, against Drug-resistant Strains of Plasmodia

2003 ◽  
Vol 56 (8) ◽  
pp. 727-729 ◽  
Author(s):  
KAZUHIKO OTOGURO ◽  
HIDEAKI UI ◽  
AKI ISHIYAMA ◽  
MIYUKI KOBAYASHI ◽  
HIDEAKI TOGASHI ◽  
...  
Keyword(s):  
Macrolide Antibiotic ◽  
Drug Resistant ◽  
Resistant Strains ◽  
Drug Resistant Strains
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