Synthesis and biological evaluation of 2-(3′-(1H-tetrazol-5-yl) bicyclo[1.1.1]pent-1-yl)glycine (S-TBPG), a novel mGlu1 receptor antagonist
Synthesis and biological evaluation of 2-(3′-(1H-tetrazol-5-yl) bicyclo[1.1.1]pent-1-yl)glycine (S-TBPG), a novel mGlu1 receptor antagonist
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DOI：
10.1016/s0968-0896(00)00270-4
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发表时间：
2001-02-01
影响因子：
3.5
通讯作者：
Pellicciari, R
中科院分区：
文献类型：
--
作者：
Costantino, G;Maltoni, K;Pellicciari, R
报道了一种新型mGluR1拮抗剂2-（3'-（1h -四唑-5-基）双环[1.1.1]-1-基）甘氨酸（S-TBPG）的设计与合成。S-TBPG的特征是2-（3'-羧基双环[1.1.1]-1-基）甘氨酸（S-CBPG）的远端羧基被四唑基部分生物等构取代。尽管效力适度降低，S-TBPG是一种选择性mGluR1拮抗剂（69 muM），对其他mCluR亚型没有活性。从mGluR1拮抗剂的构效关系（SAR）角度讨论了S-TBPG有趣的生物学特性及其独特的化学结构。2001爱思唯尔科学有限公司版权所有。
The design and synthesis of 2-(3'-(1H-tetrazol-5-yl)bicyclo[1.1.1]pent-1-yl)glycine (S-TBPG), a novel mGluR1 antagonist is reported. S-TBPG is characterized by the bioisosteric replacement of the distal carboxy group of 2-(3'-carboxybicyclo [1.1.1]pent-1-yl)glycine (S-CBPG) by a tetrazolyl moiety. Despite a moderate reduction in potency, S-TBPG is a selective mGluR1 antagonist (69 muM), with no activity at other mCluR subtypes. The interesting biological profile of S-TBPG, coupled with its peculiar chemical structure, is discussed in terms of the structure-activity relationship (SAR) of mGluR1 antagonists. (C) 2001 Elsevier Science Ltd. All rights reserved.