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Efficient Synthesis of the GABAA Receptor Agonist Trans-4-aminocrotonic Acid (TACA)

Bioorganic & medicinal chemistry letters(2017)

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摘要
Investigations into the pharmacology of different types of cys-loop GABA receptor have relied for years on the chemical modification of GABA-like compounds. The GABA metabolite GABOB is an attractive molecule to modify due to its convenient chemical structure. In the process of developing new GABA-mimic compounds from GABOB as a starting compound three small molecule GABA derivatives were synthesized using a variety of chemical transformations. Amongst these, a new and reliable method to synthesize TACA (trans-4-aminocrotonic acid) is reported.
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关键词
H. contortus,GABA,TACA,GABA(A) receptor,GABOB
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