📜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
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