CAS: 7151-76-0; 4-(Methylsulfonamido)Benzoic Acid

该化合物是一种化学化合物,其特点是芳香结构,并同时含有一种碳本体酸和磺酰胺功能组;一种白色的脱白晶状固体,可溶于水和极有机溶剂;该化合物主要用于治疗炎性肠道疾病,如肺炎,因其抗炎特性而成为宝贵的治疗剂; 磺酰胺组提高其溶性性和生物利用率,从而能够有效地向胃肠道交付; 从化学行为角度讲,4-(甲烷硫氨基)苯甲酸具有典型的酸基特性,其碳本酸组能够以水溶溶液中捐献质; 其分子结构有助于其药理活动,使其成为一种宝贵的治疗剂; 此外,必须小心处理这一化合物,因为所有化学品都遵循适当的安全准则,以降低任何健康风险.

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methyl 4-(methanesulfonylamino)benzoate 4-amino-benzoic acid methanesulfonyl chloride 4-methoxycarbonyl aniline 4-Methanesulfonylamino-N-{2-[2-(5-methyl-1H-imidazol-4-yl)-ethylamino]-ethyl}-benzamide N-{4-[4-(1-Methyl-1H-benzoimidazol-2-yl)-piperazine-1-carbonyl]-phenyl}-methanesulfonamide N-methyl-N-[2-[methyl(quinolin-2-yl)amino]ethyl]-4-[(methylsulfonyl)amino]benzamide ethyl>-4-benzamideN-methyl-N-2-ethyl-4-(methylsulfonyl)aminobenzamide

合成工艺路线路线简述

    📜4-(甲基磺酰胺)苯甲酸甲酯置于氢氧化钾体系中,用 甲醇 作为反应溶剂,化学反应 24.0H,以89%的收率获得产物4-甲磺酰氨基苯甲酸
    参考文献:Synthesis And Protein Kinase C Inhibitory Activities Of Balanol Analogues With Modification Of 4-Hydroxybenzamido Moiety
    标题:Synthesis And Protein Kinase C Inhibitory Activities Of Balanol Analogues With Modification Of 4-Hydroxybenzamido Moiety
    摘要:A Series Of Racemic Balanol Analogues With Modification Of The Benzamido Moiety Of Balanol Have Been Synthesized And Evaluated For Their Inhibitory Activities Against Human Protein Kinase C Isozymes (Pkc-Alpha,-Beta I,-Beta Ii,-Gamma,-Delta,-Epsilon,And-Eta). The Structural Modification Includes Replacement Of The 4-Hydroxyphenyl Group With Variously Substituted Phenyl Rings,Substitution Of The Amide Linkage With A Sulfonamide Or An Ester,And Replacement Of The 4-Hydroxyphenyl Substructure With A Hydroxyl Substituted Indole Or A Hydroxybenzyl Group. In General,These Analogues Were Found To Be Less Potent Than Balanol,But A Number Of Analogues Were Identified With Improved Isozyme Selectivity. The Structure-Activity Relationship Studies Of These Analogues Also Indicated That (1) The Optimal General Pkc Inhibition Requires A Free 4-Hydroxyl Group In The Benzamido Portion Of The Molecule,(2) The Amide Linkage Of The Benzamido Moiety Is Important For Pkc Inhibition,And (3) The Conformation Associated With The Benzamido Moiety Seems To Have A Profound Effect On Pkc Inhibition. The Requirement Of A Free 4-Hydroxyl Group In Conjunction With An Appropriate Conformation Of The Benzamido Moiety For Optimal Pkc Inhibition Suggests That The 4-Hydroxyphenyl Group May Be Involved In A Specific Inhibitor-Enzyme Interaction Important For Pkc Inhibition. (C) 1997 Elsevier Science Ltd.
    DOI:10.1016/s0968-0896(97)00125-9

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    ✅ COA系统入驻 | 共享模式

    合成参考文献


    参考文献:10.1126/sciadv.abf8711
    摘要:Schuller M, Correy GJ, Gahbauer S, Fearon D, Wu T, Díaz RE, Young ID, Carvalho Martins L, Smith DH, Schulze-Gahmen U, Owens TW, Deshpande I, Merz GE, Thwin AC, Biel JT, Peters JK, Moritz M, Herrera N, Kratochvil HT; QCRG Structural Biology Consortium, Aimon A, Bennett JM, Brandao Neto J, Cohen AE, Dias A, Douangamath A, Dunnett L, Fedorov O, Ferla MP, Fuchs MR, Gorrie-Stone TJ, Holton JM, Johnson MG, Krojer T, Meigs G, Powell AJ, Rack JGM, Rangel VL, Russi S, Skyner RE, Smith CA, Soares AS, Wierman JL, Zhu K, O'Brien P, Jura N, Ashworth A, Irwin JJ, Thompson MC, Gestwicki JE, von Delft F, Shoichet BK, Fraser JS, Ahel I. Fragment binding to the Nsp3 macrodomain of SARS-CoV-2 identified through crystallographic screening and computational docking. Sci Adv. 2021 Apr;7(16).
    摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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