The Synaptic Leap

Another interesting PZQ paper has come out of the cell biology group at the CNR in Rome, concerning the mode of action of PZQ. Using radioactive calcium, the group have demonstrated that calcium influx in itself is not enough to kill parasites. Pre-incubation with cytochalasin D promoted calcium influx but protected the worms from PZQ's schistosomicidal effects.

Deepak Singh has very recently started:-

THE SUBCELLULAR DRUG TRANSPORT LABORATORY (click here to visit our lab website)  

Wayne Best of Epichem has suggested an alternative route to (R)-PZQ, based on a Pictet-Spengler (PS) reaction of a chiral phenylethanolamine. This is an attractive route, since 1 to 2 should work well (good asymmetric induction) and the products resemble PZQ.

Craig Williams has suggested an interesting possibility of taking rac-PZQ and oxidising to the enediamide 2. This would then allow a catalytic, asymmetric hydrogenation to give (R)-PZQ.