CAS: 335030-80-3; (E)-3-(2-Aminopyrimidin-5-yl)Acrylic Acid

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benzyl (E)-3-(2-aminopyrimidin-5-yl)acrylate methyl (E)-3-(2-aminopyrimidin-5-yl)acrylate

📜Benzyl (E)-3-(2-Aminopyrimidin-5-yl)Acrylate置于sodium Hydroxide体系中,用 甲醇 用作溶剂,以90%的收率获得(2E)-3-(2-氨基嘧啶-5-基)丙烯酸
参考文献:发现基于氨基吡啶的细菌烯酰-Acp还原酶(fabi)抑制剂.
标题:发现基于氨基吡啶的细菌烯酰-Acp还原酶(fabi)抑制剂.
摘要:细菌烯酰-Acp还原酶(fabi)催化细菌脂肪酸生物合成的每个循环中的最后一步,是开发新型抗菌剂的有吸引力的目标.我们鉴定有效的选择性fabi抑制剂的努力始于对glaxosmithkline专有化合物的筛选,该鉴定了几种金黄色葡萄球菌fabi的小分子抑制剂.通过结合迭代化学化学和基于x射线晶体结构的设计,将这些引线之一开发为新型氨基吡啶衍生物9,一种来自金黄色葡萄球菌(ic(50)= 2.4 Microm)和嗜血杆菌的低微摩尔fabi抑制剂.流感(ic(50)= 4.2 Microm).化合物9对包括金黄色葡萄球菌(mic = 0.5 Microg / Ml)在内的几种生物具有非常好的体外抗菌活性,并且在s. 大鼠金黄色腹股沟脓肿感染模型.通过fabi过表达子和大分子合成研究,已证实9的作用方式是通过抑制fabi来抑制脂肪酸生物合成.综上所述,这些结果支持fabi作为有效的抗菌靶标,并证明了
Doi:10.1021/jm020050+

专利信息

专利号:US-9938258-B2
优先权日:2012-11-29
标 题:Substituted 2,3-dihydrobenzofuranyl compounds and uses thereof
发明人：BALOGLU ERKAN; SHECHTER SHARON; SHACHAM SHARON; MCCAULEY DILARA; SENAPEDIS WILLIAM; GOLAN GALI; KALID ORI
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to substituted 2,3-dihydrobenzofuranyl compounds, and more particularly to a compound represented by Structural Formula I: n nor a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.