Plasmodium yoelii nigeriensis (MDR)—Efficacy of Oral Pyronaridine against Multidrug-Resistant Malaria in Swiss Mice

2000 ◽  
Vol 94 (3) ◽  
pp. 190-193 ◽  
Author(s):  
Renu Tripathi ◽  
Aseem Umesh ◽  
Meenu Mishra ◽  
S.K. Puri ◽  
G.P. Dutta
Keyword(s):  
Multidrug Resistant ◽  
Plasmodium Yoelii ◽  
Swiss Mice

6-(4′-Aryloxy-phenyl)vinyl-1,2,4-trioxanes: A new series of orally active peroxides effective against multidrug-resistant Plasmodium yoelii in Swiss mice

2010 ◽  
Vol 20 (15) ◽  
pp. 4459-4463 ◽  
Author(s):  
Chandan Singh ◽  
Ved Prakash Verma ◽  
Niraj Krishna Naikade ◽  
Ajit Shankar Singh ◽  
Mohammad Hassam ◽  
...  
Keyword(s):  
Multidrug Resistant ◽  
Plasmodium Yoelii ◽  
Swiss Mice ◽  
Orally Active ◽  
Phenyl Vinyl

Novel naphthyl based 1,2,4-trioxanes: Synthesis and in vivo efficacy in the Plasmodium yoelii nigeriensis in Swiss mice

2021 ◽  
pp. 128372
Author(s):  
Manvika Karnatak ◽  
Mohammad Hassam ◽  
Murugesan Vanangamudi ◽  
Siddharth Sharma ◽  
Dinesh Kumar Yadav ◽  
...  
Keyword(s):  
Plasmodium Yoelii ◽  
In Vivo Efficacy ◽  
Swiss Mice

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 of novel 1,2,4-trioxanes and antimalarial evaluation against multidrug-resistant Plasmodium yoelii nigeriensis

2021 ◽  
pp. 128305
Author(s):  
Monika Shukla ◽  
Mohammad Hassam ◽  
Dinesh Kumar Yadav ◽  
Siddharth Sharma ◽  
Chandan Singh ◽  
...  
Keyword(s):  
Multidrug Resistant ◽  
Plasmodium Yoelii

scholarly journals Efficacy of Trovafloxacin against Penicillin-Susceptible and Multiresistant Strains of Streptococcus pneumoniae in a Mouse Pneumonia Model

1998 ◽  
Vol 42 (4) ◽  
pp. 862-867 ◽  
Author(s):  
Jean-Pierre Bédos ◽  
Véronique Rieux ◽  
Jacqueline Bauchet ◽  
Martine Muffat-Joly ◽  
Claude Carbon ◽  
...  
Keyword(s):  
Streptococcus Pneumoniae ◽  
Resistant Strain ◽  
Survival Rates ◽  
Multidrug Resistant ◽  
Pharmacokinetic Parameters ◽  
Beta Lactam ◽  
Time Curve ◽  
Swiss Mice ◽  
Resistant Strains

ABSTRACT The increasing emergence of penicillin-resistant and multidrug-resistant strains of Streptococcus pneumoniaewill create a serious therapeutic problem in coming years. Trovafloxacin is a novel naphthyridone quinolone with promising activity against S. pneumoniae, including penicillin-resistant strains (MIC for 90% of the isolates tested, 0.25 μg/ml). We compared its in vivo efficacy with that of other fluoroquinolones (ciprofloxacin, temafloxacin, and sparfloxacin) and a reference beta-lactam (amoxicillin) in a model of acute experimental pneumonia. Immunocompetent Swiss mice were infected by peroral tracheal delivery of a virulent, penicillin-susceptible strain (MIC, 0.03 μg/ml); leukopenic Swiss mice were infected with three poorly virulent, penicillin-resistant strains (MICs, 4 to 8 μg/ml) and a ciprofloxacin-resistant strain (MIC, 32 μg/ml). Treatments were started 6 h (immunocompetent mice) or 3 h (leukopenic mice) after infection. Doses ranging from 12.5 to 300 mg/kg were given at 12- or 8-h intervals for 3 days. Trovafloxacin (25 mg/kg) was the most effective agent in vivo against penicillin-susceptible and -resistant strains. Corresponding survival rates were 2- to 4-fold higher than with 50-mg/kg sparfloxacin or temafloxacin and 8- to 16-fold higher than with 100-mg/kg ciprofloxacin. The ratios of the area under the concentration-time curve to the MIC in serum and lung tissue were more favorable with trovafloxacin than with the other quinolones. Efficacy in vivo correlated with pharmacokinetic parameters. Trovafloxacin shows potential for the treatment of infections due to penicillin-susceptible and -resistant S. pneumoniae but appears to be ineffective against a ciprofloxacin-resistant strain.

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