Researchers at CIRM have synthesized and evaluated new series of original 2-aryloxy/arylamino-5-cyanobenzenesulfonylureas as thromboxane A2 receptor (TP receptor) antagonists.

Based on functional pharmacological test, several compounds were found to be as potent as the 2-arylamino-5-nitrobenzenesulfonylurea reference compound BM-573, supporting the view that the bio-isosteric replacement of the nitro group by a cyano group was tolerated.

TP receptor antagonist activity of the most promising molecules was confirmed in a platelet aggregation assay using the TP receptor agonist U-46619 as a pro-aggregant.

Three compounds were identified as leads for further non-clinical pharmacological and toxicological studies.

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