Selective angiotensin II AT(2) receptor agonists: Arylbenzylimidazole structure-activity relationships

Wu XY; Wan YQ; Mahalingam AK; Murugaiah AMS; Plouffe B; Botros M; Karlen A; Hallberg M; Gallo-Payet N; Alterman M

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Selective angiotensin II AT(2) receptor agonists: Arylbenzylimidazole structure-activity relationships

机译：选择性血管紧张素II AT（2）受体激动剂：芳基苄基咪唑结构-活性关系

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Structural alterations in the 2- and 5-positions of the first drug-like selective angiotensin II AT(2) receptor agonist (1) have been performed. The imidazole ring system was proven to be a strong determinant for the AT(2) selectivity, and with few exceptions all variations gave good AT(2) receptor affinities and with retained high AT(2)/AT(1) selectivities. On the contrary to the findings with AT(1) receptor agonists, the impact of structural modifications in the 5-position of the AT(2) selective compounds were less pronounced regarding activation of the AT(2) receptor. The butyloxyphenyl (56) and the propylthienyl (50) derivatives were found to exert a high agonistic effect as deduced from their capacity to induce neurite elongation in neuronal cells, as does angiotensin II.

机译：第一种药物样选择性血管紧张素II AT（2）受体激动剂（1）的2位和5位结构发生了变化。咪唑环系统被证明是对AT（2）选择性的强决定性因素，除少数例外，所有变化均提供了良好的AT（2）受体亲和力，并保留了较高的AT（2）/ AT（1）选择性。与AT（1）受体激动剂的发现相反，在AT（2）受体的激活方面，结构修饰在AT（2）选择性化合物5位的影响不那么明显。发现丁氧基苯基（56）和丙基噻吩基（50）衍生物具有很高的激动作用，这是由于它们在神经元细胞中诱导神经突伸长的能力所致，血管紧张素II也是如此。

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来源
《Journal of Medicinal Chemistry》 |2006年第24期|共9页
作者
Wu XY; Wan YQ; Mahalingam AK; Murugaiah AMS; Plouffe B; Botros M; Karlen A; Hallberg M; Gallo-Payet N; Alterman M;
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正文语种 eng
中图分类药学;
关键词
TYPE-2 RECEPTOR; NG108-15 CELLS; NEURONAL DIFFERENTIATION; NEURITE OUTGROWTH; AT(1) RECEPTORS; POTENT; RAT; ANTAGONISTS; EXPRESSION; AFFINITY;

机译：2型受体;NG108-15细胞;神经分化;神经胶质生长;AT（1）受体;作用力;大鼠;拮抗剂;表达;亲和力;

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1. Selective angiotensin II AT(2) receptor agonists: Arylbenzylimidazole structure-activity relationships [J] . Wu XY, Wan YQ, Mahalingam AK, Journal of Medicinal Chemistry . 2006,第24期

机译：选择性血管紧张素II AT（2）受体激动剂：芳基苄基咪唑结构-活性关系
2. Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: Identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melanocortin-4 receptor (mMC4R) [J] . Singh A., Dirain M., Witek R., Journal of Medicinal Chemistry . 2013,第7期

机译：在黑皮质素受体上结合有生物活性反向杂环的肽的结构活性关系：鉴定5800倍小鼠黑皮质素-3受体（mMC3R）选择性拮抗剂/部分激动剂对小鼠黑皮质素4受体（mMC4R）
3. Structure-activity relationships for 1-alkyl-3-(1-naphthoyl)indoles at the cannabinoid CB(1) and CB(2) receptors: steric and electronic effects of naphthoyl substituents. New highly selective CB(2) receptor agonists. [J] . Huffman JW, Zengin G, Wu MJ, Bioorganic and Medicinal Chemistry . 2005,第1期

机译：大麻素CB（1）和CB（2）受体上的1-烷基-3-（1-萘基）吲哚的结构活性关系：萘基取代基的空间和电子效应。新的高选择性CB（2）受体激动剂。
4. Structure-activity relationship studies of new cyclic MSH analogues using cloned-human melanocortin receptors lead to greater selectivity and inverse agonists [C] . Minying Cai, Paolo Grieco, Jonathan Wiens, the International Peptide Symposium . 2001

机译：使用克隆人黑素激素受体的新循环MSH类似物的结构 - 活性关系研究导致更大的选择性和反向激动剂
5. Selective GLP-1 receptor antagonists and glucagon/GLP-1 co-agonists discovered through an investigation into the structure-activity relationship in glucagon-related peptides. [D] . Patterson, James T. 2011

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6. Structure-Activity Relationships of Peptides Incorporating a Bioactive Reverse-Turn Heterocycle at the Melanocortin Receptors: Identification of a 5800-fold Mouse Melanocortin-3 Receptor (mMC3R) Selective Antagonist/Partial Agonist versus the Mouse Melanocortin-4 Receptor (mMC4R) [O] . Anamika Singh, Marvin Dirain, Rachel Witek, -1

机译：在Melanocortin受体上掺入生物逆向杂环的肽的结构-活性关系：鉴定为5800倍小鼠Melanocortin-3受体（mMC3R）选择性拮抗剂/部分激动剂与小鼠Melanocortin-4受体（mMC4R）
7. Structure-Activity Relationships within a Series of σ1 and σ2 Receptor Ligands: Identification of a σ2 Receptor Agonist (BS148) with Selective Toxicity against Metastatic Melanoma [O] . Silvia Franchini, Claudia Sorbi, Umberto Maria Battisti, 2017

机译：一系列Σ1和σ2受体配体中的结构 - 活性关系：鉴定σ2受体激动剂（BS148），具有抗转移性黑色素瘤的选择性毒性

Selective angiotensin II AT(2) receptor agonists: Arylbenzylimidazole structure-activity relationships

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