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m-Anisidine 3-methoxyphenyl bromide 3-methoxy-1-iodobenzene H-pyrazol-4-ylazo]-N-thiazol-2-yl-benzenesulfonamide4-[1-(3-methoxy-phenyl)-3,5-dimethyl-1H-pyrazol-4-ylazo]-N-thiazol-2-yl-benzenesulfonamide N-thiazol-2-yl-benzenesulfonamide4-{[1-(3-methoxy-phenyl)-3-methyl-5-oxo-1,5-dihydro-pyrazol-4-ylidene]-hydrazino}-N-thiazol-2-yl-benzenesulfonamide 6-Methoxy-3-(4-methoxyphenyl)-2-phenylindole 4-Hydroxy-3-{1-[(3-methoxy-phenyl)-hydrazono]-ethyl}-chromen-2-one 间氨基苯甲醚置于盐酸,Sodium Nitrite,Tin(Ll) Chloride体系中,用 水 作为反应溶剂,化学反应 1.5H,反应生成 3-甲氧基苯肼盐酸
参考文献:发现了以ftsz为目标的含1,3,4-恶二唑-2-酮的苯甲酰胺衍生物,可作为杀死多种mdr细菌菌株的高效药物.
标题:发现了以ftsz为目标的含1,3,4-恶二唑-2-酮的苯甲酰胺衍生物,可作为杀死多种mdr细菌菌株的高效药物.
摘要:由耐多药(mdr)病原体(例如耐甲氧西林的金黄色葡萄球菌(mrsa)和耐万古霉素的金黄色葡萄球菌(vrsa))引起的感染扩散,引起了人们对具有新作用机制的新型抗生素的需求.细菌分裂蛋白ftsz已被鉴定为可在临床上开发的新型药物靶标.作为开发靶向ftsz的抗菌剂的持续努力的一部分,我们在此描述了六种系列的新型含1,3,4-恶二唑-2-One,1,2,4-三唑-的设计,合成和生物活性.含3-One和含吡唑啉-5-One的苯甲酰胺衍生物.其中,化合物a14被发现是最有效的抗菌剂,对所有测试的革兰氏阳性菌株均优于环丙沙星,利奈唑胺和红霉素等临床药物,特别是耐甲氧西林,耐青霉素和临床分离的金黄色葡萄球菌.随后的生物学活性和对接分析研究证明,A14可以作为靶向ftsz的有效化合物.初步的sar表明了进一步优化这些新颖类似物的总体方向.综上所述,这项研究为开发新型靶向ftsz的杀菌剂提供了有希望的化学型.
DOI:10.1016/j.Bmc.2019.06.010
海关参考信息
- 2905110000-甲醇
2908199090-其他酚的卤化衍生物
2908999090-其他酚的硝化衍生物
2918290000-其他含酚基羧酸 - 💡 提示:海关信息按照顺序优先匹配,如需确认的海关信息,请参考相关资料。
- 详情请参考:📖 海关编码查询和海关进出口税则
专利信息
专利号:US-11040938-B2
优先权日:2016-07-27
标 题 :Continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts
发明人:MA BING; PAN SHUAI
权利人:SHANGHAI HYBRID—CHEM TECH; SHANGHAI HYBRID CHEM TECH
摘要:The present invention provided a continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts. Diazotization, reduction, acidic hydrolysis and salifying with acids are innovatively integrated together. Using acidic liquids of aniline or substituted aniline, diazotization reagents, reductants and acids as raw materials, phenylhydrazine derivative salts is obtained through the synthesis process, which is a three-step continuous tandem reaction including diazotization, reduction, acidic hydrolysis and salifying. The described synthesis process is a kind of integrated solutions, which is carried out in an integrated reactor. The feed inlets of the integrated reactor are continuously filled with raw materials. In the integrated reactor, diazotization, reduction, acidic hydrolysis and salifying are carried out continuously and orderly, and phenylhydrazine salts or substituted phenylhydrazine salts is obtained in the outlet of the integrated reactor without interruption. The total reaction time is no more than 20 min.
专利号:US-4267330-A
优先权日:1978-08-24
标 题 :Process for the synthesis of vincadifformine and related derivatives
发明人:KUEHNE MARTIN E
权利人:OMNIUM CHIMIQUE SA
摘要:This invention relates to the preparation of vincadifformine and related derivatives which are useful as starting material for the synthesis of vincamine and other related compounds possessing interesting psychopharmacologic properties. A N-benzyl-tetrahydro- gamma -carboline compound (III) is halogenated with t-butyl hypochlorite to obtain a haloindolenine compound which is directly treated with a metal dialkyl malonate such as thallium dialkyl malonate to provide a dialkyl 3-benzyl-1,2,3,4,5,6-hexahydroazepino (4,5-b) indole-5,5-dicarboxylate compound, said latter compound being hydrogenated to provide a dialkyl 1,2,3,4,5,6 hexahydroazepino (4,5-b) indole-5,5-dicarboxylate, said latter compound being condensed with a functionalized aldehyde, typically a haloaldehyde, to provide vincadifformine or a related derivative by passing through an intermediate compound being a salt of a dialkyl 3,3-(alkenyl)-1,2,3,4,5,6-hexahydroazepino(4,5-b) indolinium-(5,5)-dicarboxylate.
专利号:US-2016222024-A1
优先权日:2013-09-20
标 题:S-enantiomer of tetracyclic indole derivative as pbr ligands
发明人:TRIGG WILLIAM JOHN; JONES PAUL ALEXANDER
权利人:GE HEALTHCARE LTD
摘要:The present invention concerns in vivo imaging and in particular in vivo imaging of translocator protein (TSPO, formerly known as the peripheral benzodiazepine receptor). An indole-based in vivo imaging agent is provided that overcomes problems relating to known TSPO-binding radiotracers. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said precursor compound. Other aspects of the invention include a method for the synthesis of the in vivo imaging agent of the invention comprising use of the precursor compound of the invention, a kit for carrying out said method, and a cassette for carrying out an automated version of said method. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.
专利号:US-9481685-B2
优先权日:2008-10-02
标 题:Imaging neuroinflammation
发明人:WADSWORTH HARRY JOHN; SHAN BO; O'SHEA DENNIS; PASSMORE JOANNA MARIE; TRIGG WILLIAM JOHN
权利人:WADSWORTH HARRY JOHN; SHAN BO; O'SHEA DENNIS; PASSMORE JOANNA MARIE; TRIGG WILLIAM JOHN; GE HEALTHCARE LTD
摘要:The present invention concerns in vivo imaging and in particular in vivo imaging of the peripheral benzodiazepine receptor (PBR). A tetracyclic indole in vivo imaging agent is provided that binds with high affinity to PBR, has good uptake into the brain following administration, and which preferentially binds to tissues expressing higher levels of PBR. The present invention also provides a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. A cassette for the automated synthesis of the in vivo imaging agent is also provided. In addition, the invention provides a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, as well as methods for the use of said in vivo imaging agent.
专利号:US-2019152896-A1
优先权日:2016-07-27
标题 :Continuous Flow Process For the Synthesis of Phenylhydrazine Salts and Substituted Phenylhydrazine Salts
专利号:CA-1142178-A
优先权日:1978-08-24
标 题 :Process for the synthesis of vincadifformine and relatd derivatives