Fig. 1: Bicyclic azetidines are potent inhibitors of T. gondii tachyzoite growth. | Nature Communications

Fig. 1: Bicyclic azetidines are potent inhibitors of T. gondii tachyzoite growth.

From: Bicyclic azetidines target acute and chronic stages of Toxoplasma gondii by inhibiting parasite phenylalanyl t-RNA synthetase

Fig. 1: Bicyclic azetidines are potent inhibitors of T. gondii tachyzoite growth.The alternative text for this image may have been generated using AI.

a Rank order based on median effective concentration (EC50) determination of compounds from the bicyclic azetidine series against growth of T. gondii tachyzoites in vitro. Values represent average of two biological replicates used to calculate the EC50 value with 10-point dose–response curves. The four most potent compounds are highlighted: BRD2987 (0.0195 μM, green); BR7929 (0.0226 μM, red); BRD3444 (0.0289 μM, blue) and BRD8494 (0.0348 μM, purple). Pyrimethamine (0.248 μM, open circle) highlighted for reference. A stepwise description of chemical synthesis scheme for BRD2987 is found in Fig. S1. A complete list of EC50 values for all 28 bicyclic azetidines screened is found in Table S1. b Chemical structures of most potent bicyclic azetidines: BRD2987, BRD7929, BRD3444, and BRD8494, which differ only in the nature of appendages (R1, R2) as indicated. Source data are provided as a Source Data file.

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