Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
本文描述的化合物的化学式(I)是p38 MAPK抑制剂,可用作抗炎药物,用于治疗呼吸道疾病等疾病。
[EN] KINASE INHIBITORS<br/>[FR] INHIBITEURS DE KINASES
申请人:CHIESI FARMA SPA
公开号:WO2013083606A1
公开(公告)日:2013-06-13
Compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
N-alkylthio beta-lactams, alkyl-coenzyme a asymmetric disulfides, and aryl-alkyl disulfides as anti-bacterial agents
申请人:Turos Edward
公开号:US20080182815A1
公开(公告)日:2008-07-31
The present invention provides N-alkylthio β-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and method of their use as anti-bacterial agents.
[EN] KINASE INHIBITORS<br/>[FR] INHIBITEURS DE KINASE
申请人:CHIESI FARMA SPA
公开号:WO2014195402A1
公开(公告)日:2014-12-11
This invention relates to compounds and compositions that are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
这项发明涉及抑制p38 MAPK的化合物和组合物,可用作抗炎药物,用于治疗呼吸道疾病等疾病。
Unsymmetric aryl–alkyl disulfide growth inhibitors of methicillin-resistant Staphylococcus aureus and Bacillus anthracis
作者:Edward Turos、Kevin D. Revell、Praveen Ramaraju、Danielle A. Gergeres、Kerriann Greenhalgh、Ashley Young、Nalini Sathyanarayan、Sonja Dickey、Daniel Lim、Mamoun M. Alhamadsheh
DOI:10.1016/j.bmc.2008.05.032
日期:2008.7.1
attack on the disulfide bond. Small alkyl residues on the other sulfur provide the best activity as well, which for different bacteria appears to be somewhat dependent on the nature of the alkyl moiety. The mechanism of action of these lipophilic disulfides is likely similar to that of previously reported N-thiolated beta-lactams, which have been shown to produce alkyl-CoA disulfides through a thiol-disulfide
本研究描述了合成生产的混合芳烷基二硫化物化合物的抗菌特性,作为控制金黄色葡萄球菌和炭疽芽孢杆菌生长的一种手段。其中一些化合物具有很强的体外生物活性。我们的结果表明,在检查的 12 种不同的芳基取代基中,硝基苯基衍生物提供最强的抗生素活性。这可能是芳硫基部分作为离去基团对二硫键进行亲核攻击的电子活化的结果。其他硫上的小烷基残基也提供最佳活性,对于不同的细菌,这似乎在某种程度上取决于烷基部分的性质。这些亲脂性二硫化物的作用机制可能与之前报道的 N-硫醇化 β-内酰胺相似,已显示通过细胞质内的硫醇-二硫化物交换产生烷基-CoA 二硫化物,最终抑制 II 型脂肪酸合成。然而,混合的烷基辅酶 A 二硫化物本身没有抗菌活性,可能是由于高极性化合物不能穿过细菌细胞膜。已发现这些结构简单的二硫化物可抑制 β-酮酰基-酰基载体蛋白合酶 III 或 FabH(II 型脂肪酸生物合成中的关键酶),因此可作为开发针对