CAS: 2491-38-5; 2-Bromo-1-(4-Hydroxyphenyl)Ethanone

上下游产品

对羟基苯乙酮 4-Hydroxyacetophenone 99-93-4
4-羟基苯丙酮 4-Hydroxypropiophenone 70-70-2
4-乙酰氧基苯并酮 4-Acetyloxyacetophenone 13031-43-1

对羟基苯乙酮置于copper(Ll) Bromide体系中,用 乙酸乙酯 用作溶剂,化学反应 3.0H,以73%的收率获得2-溴-4'-羟基苯乙酮
参考文献:N-(5-Phenylthiazol-2-yl) 丙烯酰胺作为新型强效谷胱甘肽 S-转移酶 Omega 1 抑制剂的基于结构的设计.
标题:N-(5-Phenylthiazol-2-yl) 丙烯酰胺作为新型强效谷胱甘肽 S-转移酶 Omega 1 抑制剂的基于结构的设计.
摘要:使用报道的谷胱甘肽 S-转移酶 Omega 1 (Gsto1-1) 共晶结构,我们设计并合成了与催化位点上的 Cys32 共价结合的含丙烯酰胺化合物.从噻唑衍生物 10 (Gsto1-1 Ic50 = 0.6 μm) 开始,合成化合物 18 并与 Gsto1 共结晶.对命中化合物 10 的酰胺部分的修饰显着增加了 Gsto1-1 抑制效力.我们解决了带有与 Gsto1 结合的酰胺侧链的新衍生物 37 和 44 的共晶结构.与 18 相比,这些新结构显示了抑制剂 37 和 44 的苯基噻唑核心的重新定向.在 Gsto1:44 的共晶结构的指导下,设计了类似物 49,从而产生了最有效的 Gsto1-1 抑制剂(ic50 = 0.22 +/-0.02 Nm) 迄今为止已知.
Doi:10.1021/acs.Jmedchem.8B01960

专利信息

专利号:US-8906915-B2
优先权日:2009-12-17
标 题:Compounds, compositions, and methods for controlling biofilms
发明人：DE KEERSMAECKER SIGRID; DE VOS DIRK; ERMOLATEV DENIS; STEENACKERS HANS; VAN DER EYCKEN ERIK; VANDERLEYDEN JOZEF; SAVALIYA BHARAT S
权利人:DE KEERSMAECKER SIGRID; DE VOS DIRK; ERMOLATEV DENIS; STEENACKERS HANS; VAN DER EYCKEN ERIK; VANDERLEYDEN JOZEF; SAVALIYA BHARAT S; UNIV LEUVEN KATH
摘要:The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2-a]pyrimidinium salts in combination with excipients. Methods for inhibiting or controlling microbial biofilm formation in a plant, a body part of a human or an animal, or a surface with which a human or an animal may come into contact are also disclosed.

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