Orally active 1,2,4-trioxanes: Synthesis and antimalarial assessment of a new series of 9-functionalized 3-(1-arylvinyl)-1,2,5-trioxaspiro[5.5]undecanes against multi-drug-resistant Plasmodium yoelii nigeriensis in mice

Journal of Medicinal Chemistry

Volumn 49, Issue 9, 2006, Pages 2794-2803

  Singh, Chandan ^a   Malik, Heetika ^a   Puri, Sunil K ^a  

^a CENTRAL DRUG RESEARCH INSTITUTE   (India)

Author keywords

[No Author keywords available]

Indexed keywords

1,2,4 TRIOXANE DERIVATIVE; [3 [1 (4 CHLOROPHENYL)VINYL] 1,2,5 TRIOXASPIRO[5.5]UNDEC 9 YLIDENE]ACETIC ACID ETHYL ESTER; [3 [1 (4 TOLYLVINYL)] 1,2,5 TRIOXASPIRO[5.5]UNDEC 9 YLIDENE]ACETIC ACID ETHYL ESTER; ANTIMALARIAL AGENT; ARTEETHER; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIMALARIAL ACTIVITY; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DOSE TIME EFFECT RELATION; DRUG ACTIVITY; DRUG EFFECT; MOUSE; MULTIDRUG RESISTANCE; NONHUMAN; PLASMODIUM YOELII; PLASMODIUM YOELII NIGRIENSIS; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; AMINATION; ANIMALS; ANTIMALARIALS; ARTEMISININS; DRUG RESISTANCE, MULTIPLE; HETEROCYCLIC COMPOUNDS; MALARIA; MICE; MOLECULAR STRUCTURE; PLASMODIUM YOELII; STRUCTURE-ACTIVITY RELATIONSHIP; SURVIVAL RATE;

EID: 33646459918     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm051130r     Document Type: Article

References (39)

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35. 15 The treated mice surviving beyond day 28 were recorded as the mice protected by the drug. Mice treated with β-arteether served as positive controls.
36. (a) 100% suppression of parasitemia means, number of parasites if at all present, are below the detection limit. The parasites present below the detection limit can multiply and eventually can be detected. In such cases though the drug is providing near 100% suppression of the parasitemia but will not provide full protection to the treated mice. Multi-drug-resistant Plasmodium yoelii nigeriensis used in this study is resistant to chloroquine, mefloquine and halofantrine.
37. (b) 100% protection means all the treated mice survive till day 28. Similarly 60% protection means only 60% of the treated survive till day 28.
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