Chroman-3-amides as potent Rho kinase inhibitors.

Chen YT; Bannister TD; Weiser A; Griffin E; Lin L; Ruiz C; Cameron MD; Schurer S; Duckett D; Schroter T; LoGrasso P; Feng Y

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Chroman-3-amides as potent Rho kinase inhibitors.

机译：Chroman-3-amides作为有效的Rho激酶抑制剂。

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Inhibition of Rho kinase (ROCK) is an attractive strategy for the treatment of diseases such as hypertension, glaucoma, and cancer. Here we report chroman-3-amides as highly potent ROCK inhibitors with sufficient kinase selectivity, excellent cell activity, good microsomal stability, and desirable pharmacokinetic properties for study as potential therapeutic agents.

机译：抑制Rho激酶（ROCK）是一种治疗高血压，青光眼和癌症等疾病的有吸引力的策略。在这里，我们报道了色氨酸-3-酰胺作为高效的ROCK抑制剂，具有足够的激酶选择性，出色的细胞活性，良好的微粒体稳定性和理想的药代动力学特性，可作为潜在的治疗剂进行研究。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2008年第24期|共4页
作者
Chen YT; Bannister TD; Weiser A; Griffin E; Lin L; Ruiz C; Cameron MD; Schurer S; Duckett D; Schroter T; LoGrasso P; Feng Y;
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正文语种 eng
中图分类药学;生物化学;
关键词
Phosphotransferases; inhibitors; Amides; strategy; Assault by stabbing; 磷酸转移酶类; 酰胺类;

机译：Phosphotransferases;inhibitors;Amides;strategy;Assault by stabbing;磷酸转移酶类;酰胺类;

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1. Chroman-3-amides as potent Rho kinase inhibitors. [J] . Chen YT, Bannister TD, Weiser A, Bioorganic and Medicinal Chemistry Letters . 2008,第24期

机译：Chroman-3-amides作为有效的Rho激酶抑制剂。
2. Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account. [J] . Wu F, Buttner FH, Chen R, Bioorganic and Medicinal Chemistry Letters . 2010,第11期

机译：取代的2H-异喹啉-1-酮作为有效的RHO-激酶抑制剂。第1部分：命中账户。
3. Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account. [J] . Wu F, Buttner FH, Chen R, Bioorganic and Medicinal Chemistry Letters . 2010,第11期

机译：取代的2H-异喹啉-1-酮作为有效的RHO-激酶抑制剂。第1部分：命中账户。
4. Taking Quinazoline as a General Support-Nog to Design Potent and Selective Kinase Inhibitors: Application to FMS-like Tyrosine Kinase 3 [C] . Wei-Wei Li, Luo-Ding Yu, Li-Juan Chen, ICMSI;International conference of molecular simulations and applied informatics technologies . 2010

机译：以喹唑啉作为一般支持物来设计有效和选择性激酶抑制剂：在类似FMS的酪氨酸激酶3中的应用
5. Biochemical Characterization of FIKK Kinase from Cryptosporidium parvum and Discovery of Potent Inhibitors. [D] . Osman, Khan Tanjid. 2016

机译：小隐隐孢子虫FIKK激酶的生化特征和有效抑制剂的发现。
6. Discovery of Novel N-Substituted Prolinamido Indazoles as Potent Rho Kinase Inhibitors and Vasorelaxation Agents [O] . Yangyang Yao, Renze Li, Xiaoyu Liu, 2017

机译：发现新型N-取代的脯氨酰吲唑作为有效的Rho激酶抑制剂和血管舒张剂
7. Advances in tetrahydropyrido[1,2-a]isoindolone (valmerins) series: Potent glycogen synthase kinase 3 and cyclin dependent kinase 5 inhibitors. [O] . Boulahjar, Rajâa, Ouach, Aziz, Bourg, Stéphane, 2015

机译：四氢吡啶并[1,2-a]异吲哚啉酮（valmerins）系列的进展：强力糖原合酶激酶3和细胞周期蛋白依赖性激酶5抑制剂。

Chroman-3-amides as potent Rho kinase inhibitors.

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