Neuroprotection assay

Table 1 Summary of physical constants of selected experimental agents and their corresponding EC50 data derived from the Neuroprotection Assay...

A 24-hour incubation with a fresh solution of Ap, 42 (15 xM) increased ThT fluorescence by 30- to 50-fold relative to control. Phenolic compounds that displayed neuroprotective ability were able to abolish increase in ThT fluorescence assay, whereas EC and EGC were ineffective results are summarized in Table 6.2. 

Two different chiral auxiliary approaches have been applied to the synthesis of NPS 1407 and it s enantiomer (119) (147). NPS 1407 is an antagonist of the glutamate NMDA receptor that has in vivo activity in neuroprotection and anti-convulsant assays. The J2-en-antiomer was synthesized in four steps from (116)with the chiral center introduced by. a completely stereoselective alkylation of hydra-zone (117). The chiral auxiliary, jS-( )-l-ami-no-2-(methoxylmethyl)pyrrolidine (SAMP), was introduced by condensation with aldehyde (116) and removed by catalytic hydro-genolysis. In the second method, the S-enan-tiomer was formed in a four-step sequence with the chiral center installed by the Michael addition of chiral amine (121) (formed in one step from the readily available a-methylben-zylamine) to benzyl crotonate (120). NPS 1407 (123) was found to be 12 times more potent than it s enantiomer (119)at the NMDA receptor in an in vitro assay. 

---