Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists

HasegawaF.; NiidomeK.; MigihashiC.; MurataM.; NegoroT.; MatsumotoT.; KatoK.; FujiiA.

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Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists

机译：呋喃-2-碳酰肼作为口服活性胰高血糖素受体拮抗剂的发现

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Furan-2-carbohydrazides were found as orally active glucagon receptor antagonists. Starting from the hit compound 5, we successfully determined the structure activity relationships of a series of derivatives obtained by modifying the acidity of the phenol. We identified the ortho-nitrophenol as a good scaffold for glucagon receptor inhibitory activity. Our efforts have led to the discovery of compound 7l as a potent glucagon receptor antagonist with good bioavailability and satisfactory long half-life.

机译：发现呋喃-2-碳酰肼为口服活性胰高血糖素受体拮抗剂。从命中化合物5开始，我们成功地确定了通过改变酚的酸度获得的一系列衍生物的结构活性关系。我们确定邻硝基苯酚是胰高血糖素受体抑制活性的良好支架。我们的努力导致发现化合物7l作为有效的胰高血糖素受体拮抗剂，具有良好的生物利用度和令人满意的长半衰期。

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《Bioorganic and Medicinal Chemistry Letters》 |2014年第17期|共5页
作者
HasegawaF.; NiidomeK.; MigihashiC.; MurataM.; NegoroT.; MatsumotoT.; KatoK.; FujiiA.;
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正文语种 eng
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Furan-2-carbohydrazide; Glucagon; Glucagon receptor antagonist; Hyperglucagonemia; Type 2 diabetes;

机译：呋喃-2-碳酰肼;胰高血糖素;胰高血糖素受体拮抗剂;高血糖素血症;2型糖尿病;

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专利

1. Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists [J] . HasegawaF., NiidomeK., MigihashiC., Bioorganic and Medicinal Chemistry Letters . 2014,第17期

机译：呋喃-2-碳酰肼作为口服活性胰高血糖素受体拮抗剂的发现
2. Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core. [J] . Shen DM, Brady EJ, Candelore MR, Bioorganic and Medicinal Chemistry Letters . 2011,第1期

机译：发现含有吡唑核心的新型，有效，选择性和口服活性的人胰高血糖素受体拮抗剂。
3. Discovery of potent, orally active benzimidazole glucagon receptor antagonists. [J] . Kim RM, Chang J, Lins AR, Bioorganic and Medicinal Chemistry Letters . 2008,第13期

机译：发现有效的口服活性苯并咪唑胰高血糖素受体拮抗剂。
4. Monitoring Glucagon and Glucagon Antagonist-Mediated Internalization: A Useful Approach to Study Glucagon Receptor Pharmacology [C] . Pallavi Sachdev, Laxmi Manohar Tirunagari, Dennis Kappei American Peptide Symposium . 2009

机译：监测胰高血糖素和胰高血糖素拮抗剂介导的内化：研究胰高血糖素受体药理学的一种有用方法
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

机译：通过研究胰高血糖素相关肽的结构-活性关系，发现了选择性的GLP-1受体拮抗剂和胰高血糖素/ GLP-1共激动剂。
6. Asymmetric Synthesis of Conformationally Constrained Fingolimod Analogues—Discovery of an Orally Active Sphingosine 1-Phosphate Receptor Type-1 Agonist and Receptor Type-3 Antagonist [O] . Ran Zhu, Ashley H. Snyder, Yugesh Kharel, -1

机译：构象受限的芬戈莫德类似物的不对称合成—发现口服活性的鞘氨醇1-磷酸受体1型激动剂和受体3型拮抗剂。
7. Asymmetric Synthesis of Conformationally Constrained Fingolimod Analogues—Discovery of an Orally Active Sphingosine 1-Phosphate Receptor Type-1 Agonist and Receptor Type-3 Antagonist [O] . Ran Zhu, Ashley H. Snyder, Yugesh Kharel, 2007

机译：构象限制的Fingolimod类似物的不对称合成 - 发现口服活性鞘氨酸1-磷酸酯型-1激动剂和受体类型-3拮抗剂的发现
8. Discovery of Peptidomimetric Antagonists of Estrogen Receptor - Coactivator Interactions: A Novel Strategy to Combat Tamoxifen Drug Resistance. [R] . 2001

机译：发现雌激素受体 - 共激活因子相互作用的肽模拟拮抗剂：一种对抗他莫昔芬耐药性的新策略。

Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists

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