Late Stage Gametocyte Assay for Arylpyrroles

Published by MatTodd on 7 May 2012 - 2:13pm

Subject 

Results

Four of the arylpyrroles/near neighbors have been tested in a late stage anti-gametocyte imaging assay, with interesting results.

This assay is less usual than other malarial assays (because it is technically more challenging). See this paper for a clear description of the importance of the gametocyte stage of malaria. The upshot is that drugs targeting this form of the parasite (the late stage gametocyte) are particularly valuable because they could help prevent the transmission of malaria.

In fact in the above paper many antimalarial compounds did not display activity against LSG, with only methylene blue reaching an IC50 of 12 nM. Indeed more generally it seems that there are few compounds that have been identified with this activity.

Interestingly the novel compounds screened from the arylpyrrole set (but not the original GSK compound OSM-S-5) were highly potent (nanomolar) in this assay. The data are posted in the lab notebook. That's pretty interesting.

 

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MatTodd's picture

To see the relevance of this assay to the overall results for the arylpyrroles, see the Story So Far summary. The data provide a clear delineator between original GSK arylpyrroles and the near neighbour set (the iminothiazolidinones).