CAS: 5006-44-0; 6-Methyl-4-Oxo-4H-Chromene-2-Carboxylic Acid

上下游产品

Ethyl 6-Methyl-4-Oxo-4H-Chromene-2-Carboxylate 38322-65-5
6-Methyl-4-Oxo-4H-Chromen-2-Carbaldehyde 99851-63-5
6-Methyl-2-Cyanochromone 33543-93-0
N-[4-(Dimethylamino)Phenyl]-1-(6-Methyl-4-Oxochromen-2-yl)Methanimine Oxide 81501-70-4

📜Ethyl 6-Methyl-4-Oxo-4H-Chromene-2-Carboxylate置于水,碳酸氢钠体系中,化学反应生成 6-甲基色酮-2-羧酸
参考文献:含有酰胺基的色酮衍生物的合成,抗炎活性和构象关系研究
标题:含有酰胺基的色酮衍生物的合成,抗炎活性和构象关系研究
摘要:炎症是免疫系统对感染,损伤或刺激等各种刺激的最初生物反应.广泛的研究表明,越来越多的疾病是由炎症机制引发的.目前,抗炎药物因其治疗优势而广泛应用于临床.然而,我们也不能忽视潜在的副作用.本工作采用联合药物设计原理,设计合成了一系列以色酮为母核的酰胺类化合物.生物学评价结果表明,与阳性药物布洛芬相比,四种化合物表现出较低的ec 50值.值得注意的是,化合物5-9 对 Raw264.7 细胞中脂多糖 (Lps) 诱导的一氧化氮 (No) 的产生表现出最佳的抑制活性 (Ec 50 = 5.33 +/-0.57 μm).构效关系(Sar)表明,色酮母核5位和8位吸电子基团或6位和7位给电子基团的存在可以增强色酮的抗炎活性.分子对接研究预测了化合物与蛋白质之间的相互作用模式.此外,这些研究表明酰胺键是抗炎作用的关键基团.根据上述研究的总结,可以推断化合物5-9具有作为抗炎药物的潜力,值得进一步研究.
DOI:10.1016/j.Bmcl.2023.129539

专利信息

专利号:US-7109377-B2
优先权日:1996-10-16
标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
发明人：SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R
权利人:HARVARD COLLEGE
摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.

专利号:US-6531470-B1
优先权日:1998-01-23
标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

专利号:US-2003082830-A1
优先权日:1996-10-16
标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products

专利号:WO-0006525-A9
优先权日:1998-07-25
标题:Synthesis of combinatorial libraries of compounds reminiscent of natural products

专利号:WO-0006525-A2
优先权日:1998-07-25
标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products

专利号:US-6562844-B2
优先权日:1998-01-23
标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.