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Chemical Compound Review

Daraprim     5-(4-chlorophenyl)-6-ethyl- pyrimidine-2,4...

Synonyms: Daraclor, Malocide, Chloridin, Tindurine, pyrimethamine, ...
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Disease relevance of Malocide


Psychiatry related information on Malocide


High impact information on Malocide


Chemical compound and disease context of Malocide


Biological context of Malocide


Anatomical context of Malocide


Associations of Malocide with other chemical compounds


Gene context of Malocide

  • Interestingly, pyrimethamine-resistant strains of P. falciparum all have a common point mutation in the DHFR coding sequence (Thr/Ser 108 to Asn), which causes decreased binding of the folate analog [27].
  • Following previous work, where we found no evidence of upregulation of the dhfr-ts gene upon challenge with pyrimethamine, we investigated the expression at the protein level of the bifunctional gene product, which also carries thymidylate synthase (TS) activity [28].
  • Inhibition of parasite multiplication by pyrimethamine did not modify MCP-1 secretion [29].
  • Transfection of MRP5 into PyrR100 cells did not alter sensitivity to pyrimethamine or MTX but restored sensitivity to mercaptopurines, indicating that decreased MRP5 expression did not play a role in antifolate resistance [30].
  • CONCLUSIONS: DHFR mutations that lead to high-level in vitro resistance to pyrimethamine plus 1-2 DHPS mutations are not sufficient to induce in vivo failure of SP treatment in young children from Gabon [31].

Analytical, diagnostic and therapeutic context of Malocide

  • Derivatives of this vector were introduced into merozoites of P. berghei by electroporation, and parasites were selected for successful transformation in the rodent host on the basis of resistance to pyrimethamine [32].
  • We have also derived the sequence of the DHFR portion of the gene, by amplification using polymerase chain reaction, for the pyrimethamine-sensitive clone 3D7 and the pyrimethamine-resistant strains V-1, K-1, Csl-2, and Palo-alto [16].
  • The titration of partially purified DHFR with pyrimethamine revealed a 500-fold increase in the concentration of the drug needed to inhibit the DHFR activity by 50%, when the sensitive clone 3D7 (0.18 +/- 0.02 nM) was compared to the resistant clone 7G8 (95 +/- 16 nM) [33].
  • Pyrimethamine levels in plasma were measured by high-performance liquid chromatography [34].
  • An isocratic HPLC method for measuring pyrimethamine extracted from infant plasma is reported [35].


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