4-Cyano-5-(2-thiophenyl)-pyrazoles are high affinity CB1 receptor ligands

Altomonte Stefano; Baillie Gemma L.; Ross Ruth A.; Zanda Matteo

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4-Cyano-5-(2-thiophenyl)-pyrazoles are high affinity CB1 receptor ligands

机译：4-氰基-5-（2-噻吩基） - 吡唑是高亲和力CB1受体配体

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Pyrazoles bearing a 5-thiophenyl and a 4-cyano group were synthesised and tested for their affinity to the cannabinoid CB1 receptor showing in many cases single digit nanomolar K-i values and moderate to good selectivity towards the CB2 receptor. Some of these pyrazole ligands, such as 8g, displayed relatively low lipophilicity (experimental log P < 4) and high calculated Topological Polar Surface Area (TPSA) (>90) suggesting that these compounds may behave as peripherally restricted CB1 ligands. Furthermore, 2-fluoroethyl carboxamides 8d, 8h and 8l are interesting candidates for further development into PET tracers.

机译：合成含有5-噻吩基和4-氰基组的吡唑并测试它们对大麻素CB1受体的亲和力，显示在许多情况下单位数纳米Molar K-I值，并朝向CB2受体的中等至良好的选择性。这些吡唑配体，例如8g，显示相对低的亲脂性（实验性Log p <4）和高计算的拓扑极性表面积（TPSA）（TPSA）（> 90），表明这些化合物可以表现为外周限制的CB1配体。此外，2-氟乙基羧酰胺8d，8h和8L是有趣的候选者，用于进一步发展到PET示踪剂。

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《RSC Advances》 |2015年第18期|共10页
作者
Altomonte Stefano; Baillie Gemma L.; Ross Ruth A.; Zanda Matteo;
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Univ Aberdeen Inst Med Sci Kosterlitz Ctr Therapeut Aberdeen AB25 2ZD Scotland;

Univ Toronto Toronto ON M5S 1A8 Canada;

Univ Toronto Toronto ON M5S 1A8 Canada;

Univ Aberdeen Inst Med Sci Kosterlitz Ctr Therapeut Aberdeen AB25 2ZD Scotland;

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正文语种 eng
中图分类化学;
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1. 4-Cyano-5-(2-thiophenyl)-pyrazoles are high affinity CB1 receptor ligands [J] . Altomonte Stefano, Baillie Gemma L., Ross Ruth A., RSC Advances . 2015,第18期

机译：4-氰基-5-（2-噻吩基） - 吡唑是高亲和力CB1受体配体
2. Analogs of JHU75528, a PET ligand for imaging of cerebral cannabinoid receptors (CB1): development of ligands with optimized lipophilicity and binding affinity. [J] . Fan H, Kotsikorou E, Hoffman AF, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2009,第2期

机译：JHU75528的类似物，一种用于脑大麻素受体（CB1）成像的PET配体：开发具有最佳亲脂性和结合亲和力的配体。
3. Synthesis of (O-methyl-11C)1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-1H-pyrazole- 3-carboxylic acid piperidin-1-ylamide: a potential PET ligand for CB1 receptors. [J] . Kumar JS, Prabhakaran J, Arango V, Bioorganic and Medicinal Chemistry Letters . 2004,第10期

机译：（O-甲基-11C）1-（2-氯苯基）-5-（4-甲氧基苯基）-4-甲基-1H-吡唑-3-羧酸哌啶-1-基酰胺的合成：CB1受体的潜在PET配体。
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. Molecular Recognition of Association Processes: Assessment of Diffusional Association, Binding Pathways, and Selective Affinity in Ligand-Receptor Complexes. [D] . Roberts, Christopher Carver. 2014

机译：缔合过程的分子识别：评估配体-受体复合物中的扩散缔合，结合途径和选择性亲和力。
6. Analogs of JHU75528 a PET ligand for imaging of cerebral cannabinoid receptors (CB1): development of ligands with optimized lipophilicity and binding affinity [O] . Hong Fan, Evangelia Kotsikorou, Alexander F. Hoffman, -1

机译：JHU75528的类似物一种用于脑大麻素受体（CB1）成像的PET配体：开发具有最佳亲脂性和结合亲和力的配体
7. Evaluation of (Z)-2-((1-benzyl-1H-indol-3-yl)methylene)-quinuclidin-3-one analogues as novel, high affinity ligands for CB1 and CB2 cannabinoid receptors [O] . Nikhil Reddy Madadi, Narsimha Reddy Penthala, Lisa K. Brents, 2013

机译：评价（Z）-2 - （（1-苄基-1H-吲哚-3-基）亚甲基）-quinuclidin-3-一种类似物作为CB1和CB2大麻素受体的新型，高亲和力配体

4-Cyano-5-(2-thiophenyl)-pyrazoles are high affinity CB1 receptor ligands

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