Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.

Sessions EH; Yin Y; Bannister TD; Weiser A; Griffin E; Pocas J; Cameron MD; Ruiz C; Lin L; Schurer SC; Schroter T; LoGrasso P; Feng Y

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.

【24h】

Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.

机译：基于苯并咪唑和苯并恶唑的Rho激酶抑制剂。

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

Inhibitors of Rho kinase have been developed based on two distinct scaffolds, benzimidazoles, and benzoxazoles. SAR studies and efforts to optimize the initial lead compounds are described. Novel selective inhibitors of ROCK-II with excellent potency in both enzyme and cell-based assays were obtained. These inhibitors possess good microsomal stability, low cytochrome P-450 inhibitions and good oral bioavailability.

机译：已经基于两种不同的支架，苯并咪唑和苯并恶唑开发了Rho激酶抑制剂。描述了SAR研究和优化初始铅化合物的努力。获得了新型的ROCK-II选择性抑制剂，在酶和基于细胞的测定中均具有出色的效能。这些抑制剂具有良好的微粒体稳定性，低的细胞色素P-450抑制作用和良好的口服生物利用度。

著录项

来源
《Bioorganic and Medicinal Chemistry Letters》 |2008年第24期|共4页
作者
Sessions EH; Yin Y; Bannister TD; Weiser A; Griffin E; Pocas J; Cameron MD; Ruiz C; Lin L; Schurer SC; Schroter T; LoGrasso P; Feng Y;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类药学;生物化学;
关键词
inhibitors; Phosphotransferases; ROCK-II; Oral; 磷酸转移酶类;

机译：inhibitors;Phosphotransferases;ROCK-II;Oral;磷酸转移酶类;

相似文献

外文文献
中文文献
专利

1. Benzimidazole- and benzoxazole-based inhibitors of Rho kinase. [J] . Sessions EH, Yin Y, Bannister TD, Bioorganic and Medicinal Chemistry Letters . 2008,第24期

机译：基于苯并咪唑和苯并恶唑的Rho激酶抑制剂。
2. The Down syndrome critical region protein TTC3 inhibits neuronal differentiation via RhoA and Citron kinase. [J] . Berto G, Camera P, Fusco C, Journal of Cell Science . 2007,第Pta11期

机译：唐氏综合症关键区域蛋白TTC3通过RhoA和Citron激酶抑制神经元分化。
3. Y-27632, an inhibitor of rho-associated protein kinase, suppresses tumor cell invasion via regulation of focal adhesion and focal adhesion kinase. [J] . Imamura F, Mukai M, Ayaki M, Japanese Journal of Cancer Research . 2000,第8期

机译：Y-27632是rho相关蛋白激酶的抑制剂，可通过调节粘着斑和粘着斑激酶来抑制肿瘤细胞的侵袭。
4. Inhalable Liposomes of Fasudil-a Novel Rho-Kinase Inhibitor for the Treatment of PAH [C] . Vivek Gupta, Fakhrul Ahsan Annual meeting exposition of the Controlled Release Society . 2011

机译：法舒地尔的新型可吸入脂质体-一种新型Rho激酶抑制剂，可治疗PAH
5. Identification and characterization of a selective inhibitor of the PIM-1 kinase. [D] . Holder, Sheldon Levon. 2005

机译：PIM-1激酶选择性抑制剂的鉴定和表征。
6. Optimization of benzoxazole-based inhibitors of Cryptosporidium parvum inosine 5′-monophosphate dehydrogenase [O] . Suresh Kumar Gorla, Mandapati Kavitha, Minjia Zhang, -1

机译：基于苯并恶唑的小隐孢子肌苷5-单磷酸脱氢酶抑制剂的优化
7. Recoverin binds exclusively to an amphipathic peptide at the N terminus of rhodopsin kinase, inhibiting rhodopsin phosphorylation without affecting catalytic activity of the kinase. [O] . Higgins, MK, Oprian, DD, Schertler, GF 2006

机译：恢复蛋白仅与视紫红质激酶N末端的两亲性肽结合，从而抑制视紫红质的磷酸化而不影响该激酶的催化活性。

Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.

摘要

著录项

相似文献

相关主题

期刊订阅