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4th September 2014 @ 07:21

A further set of Series 4 Triazolopyrazine compounds have been sent to have their efficacy evaluated against Plasmodium falciparum in-vitro at Syngene.

The compounds are ethers and amides. Compounds are intended by default to have cLogP < 3.5. Those that do not are either older compounds already made, or are evaluating something specific, e.g. the prototypical ether compound OSM-S-260 or OSM-S-259 which assesses potency of benzylic ethers. Results will be posted in due course.

 

OSM Compounds Sep Syngene.png

General assay principle:
"This protocol assesses compound efficacy against Plasmodium falciparum in-vitro. This assay is using [3H]-hypoxanthine incorporation or DNA labeling by SYBR Green as a markers of parasite growth.
This procedure is designed for use with culture adapted P. falciparum strains or clones only. On one 96-well plate typically 03 drugs are tested in duplicate. Standard strains: Plasmodium falciparum, NF54 (sensitive to all known drugs), Plasmodium falciparum, K1 (chloroquine and pyrimethamine resistant). The assay can be performed in dose response mode (12 concentrations in duplicate, 24 data points) which allows determining IC50, or in single concentration mode (one concentration in triplicate, 3 data points) which allows determining the percentage of growth inhibition.
For more information, see Desjardins et al. (Antimicrob. Agents Chemother., 16(6), 710, 1979)."

 

(Post originally authored by Alice Williamson, tweaked by Mat)

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OSM Compounds Sep Syngene.cdxml
OSM Compounds Sep Syngene.png