申请人:SUNTORY LIMITED
公开号:EP0948962A2
公开(公告)日:1999-10-13
The present invention provides blockers for glutamate transporters. During a series of syntheses searching for glutamate uptake inhibition in Xenopus oocytes injected with bovine glutamate transporter genes (BGLAST), we obtained β-hydroxyaspartic acid derivatives of the following chemical formula (1):
wherein R represents an aromatic acyl group which may be substituted on the ring, a straight or branched lower aliphatic acyl group, an aryl group which may be substituted on the ring, an aralkyl group which may be substituted on the ring, or a straight or branched lower alkyl group; and salts thereof. These compounds are blockers of glutamate transporters, which are useful for the understanding of the function of glutamate transporters and show promise for the treatment of various neurodegenerative diseases.
本发明提供了谷氨酸转运体的阻断剂。在一系列寻找抑制注射了牛谷氨酸转运体基因(BGLAST)的爪蟾卵母细胞谷氨酸摄取的合成过程中,我们获得了以下化学式(1)的β-羟基天冬氨酸衍生物:
其中 R 代表环上可被取代的芳酰基、直链或支链低级脂肪酰基、环上可被取代的芳基、环上可被取代的芳烷基或直链或支链低级烷基;及其盐类。这些化合物是谷氨酸转运体的阻断剂,有助于了解谷氨酸转运体的功能,并有望治疗各种神经退行性疾病。