Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies.

Lange JH; van der Neut MA; Wals H

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Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies.

机译：新型咪唑类化合物的合成和合成孔径雷达（SAR），是具有高结合效率的强效和选择性大麻素CB2受体拮抗剂。

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The synthesis and structure-activity relationship studies of imidazoles are described. The target compounds 6-20 represent a novel chemotype of potent and CB(2)/CB(1) selective cannabinoid CB(2) receptor antagonists/inverse agonists with very high binding efficiencies in combination with favourable logP and calculated polar surface area values. Compound 12 exhibited the highest CB(2) receptor affinity (K(i)=1.03 nM) in this series, as well as the highest CB(2)/CB(1) subtype selectivity (>9708-fold).

机译：描述了咪唑的合成及其构效关系。目标化合物6-20代表有效的新型化学型和CB（2）/ CB（1）选择性大麻素CB（2）受体拮抗剂/反向激动剂，结合效率很高，并具有良好的logP和计算出的极性表面积值。在此系列中，化合物12表现出最高的CB（2）受体亲和力（K（i）= 1.03 nM），以及最高的CB（2）/ CB（1）亚型选择性（> 9708倍）。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第3期|共6页
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Lange JH; van der Neut MA; Wals H;
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1. Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies. [J] . Lange JH, van der Neut MA, Wals H Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：新型咪唑类化合物的合成和合成孔径雷达（SAR），是具有高结合效率的强效和选择性大麻素CB2受体拮抗剂。
2. Bioisosteric replacements of the pyrazole moiety of rimonabant: synthesis, biological properties, and molecular modeling investigations of thiazoles, triazoles, and imidazoles as potent and selective CB1 cannabinoid receptor antagonists. [J] . Lange JH, van Stuivenberg HH, Coolen HK, Journal of Medicinal Chemistry . 2005,第6期

机译：利莫那班吡唑部分的生物立体置换：噻唑，三唑和咪唑作为有效和选择性的CB1大麻素受体拮抗剂的合成，生物学性质和分子模型研究。
3. Evaluation of the cannabinoid CB2 receptor-selective antagonist, SR144528: further evidence for cannabinoid CB2 receptor absence in the rat central nervous system. [J] . Griffin G, Wray EJ, Tao Q, European Journal of Pharmacology: An International Journal . 1999,第1期

机译：大麻素CB2受体选择性拮抗剂SR144528的评估：大鼠中枢神经系统中大麻素CB2受体缺失的进一步证据。
4. THE ROLE OF ANANDAMIDE AND RELATED FATTY ACID ETHANOLAMIDES AS ENDOGENOUS LIGANDS FOR THE CB1 AND CB2 CANNABINOID RECEPTORS [C] . Christian C. Felder, Amie Nielsen, Eileen M. Briley, International Washington Spring Symposium . 1996

机译：Anandamide和相关脂肪酸乙醇酰胺作为CB1和CB2大麻素受体的内源配体的作用
5. Design, synthesis and biological evaluation of novel selective cannabinoid receptor 2 (CB2) ligands with therapeutic potentials. [D] . Almehizia, Abdulrahman A. 2015

机译：具有治疗潜力的新型选择性大麻素受体2（CB2）配体的设计，合成和生物学评估。
6. Sch35966 is a potent selective agonist at the peripheral cannabinoid receptor (CB2) in rodents and primates [O] . W Gonsiorek, C A Lunn, X Fan, 2007

机译：Sch35966是啮齿动物和灵长类动物外周大麻素受体（CB2）的强效选择性激动剂
7. Bioisosteric Replacements of the Pyrazole Moiety of Rimonabant: Synthesis, Biological Properties, and Molecular Modeling Investigations of Thiazoles, Triazoles, and Imidazoles as Potent and Selective CB1 Cannabinoid Receptor Antagonists [O] . -1

机译：甲嘧唑类吡唑部分的生物脑蛋白酶部分：噻唑，三唑和咪唑的合成，生物学性能和分子建模研究是有效和选择性CB1大麻素受体拮抗剂

Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies.

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