Synthesis and biological evaluation of new 2-amino-6-(trifluoromethoxy)benzoxazole derivatives, analogues of riluzole

被引：2

作者：

Calabro, Maria Luisa ^{[1
]}

Caputo, Rosanna ^{[1
]}

Ettari, Roberta ^{[2
]}

Puia, Giulia ^{[3
]}

Ravazzini, Federica ^{[3
]}

Zappala, Maria ^{[1
]}

Micale, Nicola ^{[1
]}

机构：

[1] Univ Messina, Dipartimento Sci Farmaco & Prod Salute, I-98168 Messina, Italy

[2] Univ Milan, Dipartimento Sci Farmaceut, I-20133 Milan, Italy

[3] Univ Modena & Reggio Emilia, Dipartimento Sci Biomed, Reggio Emilia, Italy

来源：

MEDICINAL CHEMISTRY RESEARCH | 2013年 / 22卷 / 12期

关键词：

2-Aminobenzoxazole derivatives; Riluzole; Patch-clamp technique; Neuronal primary cultures; Binding assays; AMYOTROPHIC-LATERAL-SCLEROSIS; NEURONS; SODIUM; MECHANISMS; RECEPTORS; GLUTAMATE; RELEASE; TRIAL; NMDA;

D O I：

10.1007/s00044-013-0594-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This manuscript describes the synthesis of a new series of 2-amino-6-(trifluoromethoxy)benzoxazole derivatives (1-5) and a benzothiazine derivative (6) structurally related to riluzole, the only neuroprotective drug currently approved for the treatment of the amyotrophic lateral sclerosis. Preliminary results indicate that the synthesized compounds, in particular benzamide derivatives 3 and 4, are able to antagonize voltage-dependent Na+ channel currents, and therefore they could be exploited as new inhibitors of these channels. Moreover, all compounds possess low binding affinity for GABA and NMDA receptors.

引用

页码：6089 / 6095

页数：7

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