A divergent asymmetric total synthesis of voacafricines and B, hexacyclic monoterpene indole alkaloids, has been accomplished featuring the following key steps: a) a catalyst-controlled Pictet–Spengler reaction 6-methoxytryptamine with chiral α-ketoester affording 1,1-disubstituted tetrahydro-β-carboline in excellent yield diastereoselectivity; b) oxidative cleavage 3,5-disubstituted cyclopente...

Intramolecular gold (I)-catalyzed cyclization of 2-alkynylindole-3-carbaldehyde oximes enabled direct construction the unknown γ-carboline N-oxide scaffold at ambient temperature. This reaction proceeded through an interesting 6-endo-dig mechanism and afforded desired products with satisfactory to high yields. The scope limitations methodology were evaluated final compounds fully characterized....

Chick brain mRNA was isolated and injected into Xenopus oocytes. This led to the expression in the surface membrane of functional GABA-activated channels with properties reminiscent of vertebrate GABAA channels. The GABA-induced current was analyzed quantitatively under voltage-clamp conditions. Picrotoxin inhibited this current in a concentration-dependent manner with IC50 = 0.6 microM. The al...