Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties

Ronald Palin; Anton Bom; John K. Clark; Louise Evans; Helen Feilden; Andrea K. Houghton; Philip S. Jones; Brian Montgomery; Mark A. Weston; Grant Wishart

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Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties

机译：具有镇痛和镇静作用的N-3取代苯氧丙基哌啶苯并咪唑-2-酮类似物作为NOP受体激动剂的合成和评价

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摘要

A series of 3-phenoxypropyl piperidine benzimidazol-2-one analogues have been discovered as novel NOP receptor agonists. Structure-activity relationships have been explored via N-3 substitution of the benzimidazol-2-one with a range of functionality. The N-methyl acetamide derivative (+)-7f was found to be a high-affinity, potent NOP agonist with greater than 100-fold selectivity over the MOP receptor. Furthermore (+)-7f was shown to be both antinociceptive and sedative when administered iv to rodents.

机译：已发现一系列3-苯氧基丙基哌啶苯并咪唑-2-酮类似物作为新型的NOP受体激动剂。通过苯并咪唑-2-酮的N-3取代具有一系列功能，已经探索了结构-活性关系。发现N-甲基乙酰胺衍生物（+）-7f是一种高亲和力的强效NOP激动剂，其选择性是MOP受体的100倍以上。此外，当对啮齿动物静脉给药时，（+）-7f被证明具有镇痛和镇静作用。

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来源
《Bioorganic and Medicinal Chemistry》 |2007年第4期|1828-1847|共20页
作者
Ronald Palin; Anton Bom; John K. Clark; Louise Evans; Helen Feilden; Andrea K. Houghton; Philip S. Jones; Brian Montgomery; Mark A. Weston; Grant Wishart;
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作者单位

Department of Chemistry, Organon Laboratories Ltd., Newhouse, Lanarkshire ML1 5SH, UK;

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原文格式 PDF
正文语种 eng
中图分类药学;生物化学;
关键词
NOP; ORLl; antinociception; analgesic; sedative; benzimidazolone;

机译：NOP;ORLl;抗伤害感受止痛药镇静剂;苯并咪唑酮;

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1. Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties. [J] . Palin R, Bom A, Clark JK, Bioorganic and medicinal chemistry . 2007,第4期

机译：具有镇痛和镇静作用的N-3取代的苯氧基丙基哌啶苯并咪唑-2-酮类似物作为NOP受体激动剂的合成和评价。
2. Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties. [J] . PalinR, BomA, ClarkJK, Bioorganic and Medicinal Chemistry . 2007,第4期

机译：具有镇痛和镇静作用的N-3取代的苯氧基丙基哌啶苯并咪唑-2-酮类似物作为NOP受体激动剂的合成和评价。
3. Structure-activity relationships and CoMFA of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic properties. [J] . Palin R, Clark JK, Evans L, Bioorganic and medicinal chemistry . 2008,第6期

机译：N-3取代苯氧丙基哌啶苯并咪唑-2-酮类似物作为具有镇痛作用的NOP受体激动剂的结构活性关系和CoMFA。
4. Design, synthesis and biological evaluation of novel fentanyl analogues as agonist of μ-opioid receptor [C] . LIU Ming, HU Wen-xiang International Conference on Advanced Design and Manufacturing Engineering . 2012

机译：新型芬太尼类似物作为μ-ApiOID受体激动剂的设计，合成和生物学评价
5. Synthesis of new glutamate receptor probes: I. Total synthesis of dysiherbaine, a potent glutamate receptor excitotoxin; II. Design and synthesis of dysiherbaine analogues; III. Synthesis and structure-activity relationships of substituted benzothiadiazides and their role as AMPA receptor modulators. [D] . Phillips, Dean Paul. 2001

机译：新型谷氨酸受体探针的合成：I. dysiherbaine的全合成，一种有效的谷氨酸受体兴奋性毒素；二。 dysiherbaine类似物的设计和合成；三，取代的苯并噻二叠氮化物的合成及其构效关系及其作为AMPA受体调节剂的作用。
6. Functional plasticity of the N/OFQ-NOP receptor system determines analgesic properties of NOP receptor agonists [O] . W Schröder, D G Lambert, M C Ko, 2014

机译：N / OFQ-NOP受体系统的功能可塑性决定了NOP受体激动剂的镇痛特性
7. Functional plasticity of the N/OFQ-NOP receptor system determines analgesic properties of NOP receptor agonists [O] . W Schröder, D G Lambert, M C Ko, 2014

机译：N / Q-NOP受体系统的功能可塑性确定NOP受体激动剂的镇痛性
8. Pharmacological Studies of NOP Receptor Agonists as Novel Analgesics [R] . Ko, M. 2010

机译：NOp受体激动剂作为新型镇痛药的药理学研究

Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties

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