CAS: 127-71-9; N-((4-Aminophenyl)Sulfonyl)Benzamide

该化合物是一种具有细菌特性的磺胺抗生素,主要对广泛的抗克菌阳性和克菌阴性细菌有效,其行动机制包括竞争抑制丙氨基苯酸(PABA),干扰细菌叶酸合成并阻碍核酸生产.硫化苯并二氮胺通常用于治疗细菌感染的时用配方,特别是在皮肤和合成生态应用中,因为其局部效力和系统吸收率较低.其水溶剂的稳定性以及与其他抗微生物剂的兼容性增强了其复合制剂的效用.该化合物有详细记载的药用植物基因特征和微弱抗药性发展进一步支持其在临床环境中继续使用.

结构式图片

相似化合物

6971-74-0 120336-96-1 14068-01-0

欧盟法规

ECHA物质ECHA物质C&L通报REACH预注册

上下游产品

CAS号93-99-2 苯甲酸苯酯 | CAS号63-74-1 磺胺 | CAS号5661-33-6 N-benzoyl-4-(ac... | CAS号98-88-4 苯甲酰氯 | CAS号121-61-9 4-乙酰氨基苯磺酰胺 | CAS号724423-50-1 N-benzoyl-sulfa... | CAS号55871-46-0 benzyl N-(4-sul... | CAS号65-85-0 苯甲酸 | CAS号623-11-0 对硝基甲苯

合成工艺路线路线简述

  • 合成目标产物 Sulfabenzamide 主要起始原料 Benzoyl Chloride
  • (文献来源)合成步骤主要原料 Benzoyl Chloride
N-苯甲酰基-4-(乙酰氨基)苯磺酰胺置于盐酸体系中,化学反应 2.0H,反应生成苯甲酰磺胺
参考文献:孤儿g蛋白偶联受体gpr27激动剂的构效关系
标题:孤儿g蛋白偶联受体gpr27激动剂的构效关系
摘要:Gpr27 与 Gpr85 和 Gpr173 一起属于三个受体的小亚家族,称为"大脑中表达的超保守受体"(sreb).它被假定参与关键的生理过程,如神经元可塑性,能量代谢和胰腺 β 细胞胰岛素分泌和调节.最近,我们报道了第一个选择性 Gpr27 激动剂,2,4-二氯-N-(4-( N-苯基氨磺酰基)苯基)苯甲酰胺 ( I,Pec 50 6.34,E Max 100%).在这里,我们描述了i的一系列新衍生物和类似物的合成和构效关系: 在抑制蛋白募集测定中评估了所有产品激活 Gpr27 的能力.结果,确定了具有广泛功效的激动剂,包括部分激动剂和完全激动剂,显示出比先导化合物i更高的功效.最有效的激动剂是 4-Chloro-2,5-Difluoro-N-(4-( N-Phenylsulfamoyl)Phenyl)Benzamide ( 7Y,Pec 50 6.85,E Max
Doi:10.1016/j.Ejmech.2021.113777

海关参考信息

专利信息


专利号:US-9693999-B2
优先权日:2011-01-26
标题:Small molecule RNase inhibitors and methods of use
发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE
权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education
摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.

专利号:US-9439423-B2
优先权日:2007-10-29
标 题 :Antiparasitic agent for fish and method of controlling proliferation of fish parasites
发明人:KAWANO FUMI; HIRAZAWA NORITAKA
权利人:KAWANO FUMI; HIRAZAWA NORITAKA; NIPPON SUISAN KAISHA LTD
摘要:An antiparasitic agent for fish includes an inhibitor of folate synthesis and/or an inhibitor of folate activation as the active substance(s). A combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is disclosed. Sulfonamide is disclosed as suitable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist are disclosed as suitable inhibitors of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is effective against fish parasites belonging to the ciliate group.

专利号:US-9265777-B2
优先权日:2009-04-27
标题 :Antiparasitic agent for fish and method of controlling proliferation of fish parasites
发明人:KAWANO FUMI; HIRAZAWA NORITAKA
权利人:KAWANO FUMI; HIRAZAWA NORITAKA; NIPPON SUISAN KAISHA LTD
摘要:A method of controlling proliferation of fish parasites comprising the administration of 1 to 50 mg/kg fish body weight/day of an inhibitor of folate synthesis and/or an inhibitor of folate activation to fish continuously for 1 to 2 weeks. Using a combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is particularly effective against parasites belonging to the ciliate group among fish parasites.

专利号:US-2007203079-A1
优先权日:2005-11-21
标题:Methods of using small molecule compounds for neuroprotection
发明人:CALDWELL GUY A; CALDWELL KIM A; CAO SONGSONG
权利人:CALDWELL GUY A; CALDWELL KIM A; CAO SONGSONG
摘要:Methods are provided for preventing neurodegeneration and neuronal loss by administering compositions comprising small molecule compounds with the effect of preventing neurodegeneration and neuronal loss. In one aspect of the invention, the methods and compositions are also useful for treating neurodegenerative diseases. Small molecule compounds provide an important treatment option because of their stability, ease of use in both manufacture and formulation, ease of administration, and patient compliance. The small molecule compound compositions of the present invention may include topoisomerase II inhibitors, bacterial transpeptidase inhibitors, calcium channel antagonists, cyclooxygenase inhibitors, folic acid synthesis inhibitors, or sodium channel blockers and functional analogues thereof that have an effect on neurodegeneration. The compositions of the present invention may be administered prophylactically before the onset of clinical symptoms or after clinical symptoms of a neurodegenerative disease have manifested.

专利号:US-6103865-A
优先权日:1998-08-03
标 题 :PH-sensitive polymer containing sulfonamide and its synthesis method
发明人:BAE YOU HAN; PARK SANG YEOB
权利人:KWANGJU INST SCI & TECH
摘要:There are disclosed pH-sensitive polymers containing sulfonamide groups, which can be changed in physical properties, such as swellability and solubility, depending on pH and which can be applied for a drug-delivery system, bio-material, sensor, etc, and a preparation method therefor. The pH-sensitive polymers are prepared by introduction of sulfonamide groups, various in pKa, to hydrophilic groups of polymers either through coupling to the hydrophilic groups, such as acrylamide, N,N-dimethylacrylamide, acrylic acid, N-isopropylacrylamide, etc, of polymers or copolymerization with other polymerizable monomers. These pH-sensitive polymers may have a structure of linear polymer, grafted copolymer, hydrogel or interpenetrating network polymer.

专利号:WO-2009056955-A1
优先权日:2007-10-30
标题 :Amine-bearing phospholipids (abps), their synthesis and use
发明人:ZUMBUEHL ANDREAS
权利人:UNIV BASEL; ZUMBUEHL ANDREAS
摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
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主要参考文献

[参考文献]: Rostamizadeh S, Et, Al. Synthesis Of Sulfamethoxazole And Sulfabenzamide Metal Complexes; Evaluation Of Their Antibacterial Activity. Eur J Med Chem. 2019 Jun 1;171:364-371.
[参考文献]: Ahmad G Nozad, Et Al. A Systematic Study On Hydrogen Bond Interactions In Sulfabenzamide: Dft Calculations Of The N-14, O-17, And H-2 Nqr Parameters. Biophys Chem. 2009 Feb;139(2-3):116-22.
[参考文献]: B M Jones, Et Al. In Vitro Susceptibility Of Gardnerella Vaginalis And Bacteroides Organisms, Associated With Nonspecific Vaginitis, To Sulfonamide Preparations. Antimicrob Agents Chemother. 1982 Jun;21(6):870-2.
[参考文献]: C A Spinks, Et Al. Molecular Modeling Of Hapten Structure And Relevance To Broad Specificity Immunoassay Of Sulfonamide Antibiotics. Bioconjug Chem. 1999 Jul-Aug;10(4):583-8.
[参考文献]: Giorgio Ottaviani, Et Al. In Silico And In Vitro Filters For The Fast Estimation Of Skin Permeation And Distribution Of New Chemical Entities. J Med Chem. 2007 Feb 22;50(4):742-8.

合成参考文献


摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664
参考文献:10.1002/bies.10114
摘要:Bermingham A, Derrick JP. The folic acid biosynthesis pathway in bacteria: evaluation of potential for antibacterial drug discovery. Bioessays. 2002 Jul;24(7):637–48. doi: 10.1002/bies.10114.
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