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A new synthetic method and GABA transporter inhibitory activities of Tiagabine and its analogues are described. The key intermediates 4-tosyl-1,1-diaryl/heteroaryl-1-butene 10a—10e were synthesized by Wittig reaction, and followed by N-alkylation with (R)-3-piperidinecarboxylate. The resulting N-diheterocyclylalkenylpiperidine-3-carboxylic acid ester [STHZ]11a—11e[STBZ] were saponified and then acidified to get the target compounds [STHZ]1a—1e[STBZ]. The preliminary bioassays show that compound [STHZ]1a—1e[STBZ] exhibited excellent inhibition of [ 3H]-GABA uptake in vitro of culture cells.=
A new synthetic method and GABA transporter inhibitory activities of Tiagabine and its analogues are described. The key intermediates 4-tosyl-1,1-diaryl / heteroaryl-1-butene 10a-10e were synthesized by Wittig reaction, and followed by N-alkylation with (R) -3-piperidinecarboxylate. The resulting N-diheterocyclylalkenylpiperidine-3-carboxylic acid ester [STHZ] 11a-11e [STBZ] were saponified and then acidified to get the target compounds [STHZ] 1a-1e [STBZ] Preliminary bioassays show that compound [STHZ] 1a-1e [STBZ] exhibited excellent inhibition of [3H] -GABA uptake in vitro of culture cells.