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CAS号60677-14-7 3-苯氧基苯甲酸乙酯 | CAS号3586-14-9 3-苯氧基甲苯 | CAS号39515-51-0 间苯氧基苯甲醛 | CAS号74482-46-5 3-phenoxybenzal... | CAS号75-91-2 叔丁基过氧化氢 | CAS号13826-35-2 3-苯氧基苄醇 | CAS号7781-98-8 3-羟基苯甲酸乙酯 | CAS号127-09-3 乙酸钠 | CAS号98-80-6 苯硼酸 | CAS号2974-95-0 1-Iodo-3-phenox... | CAS号101-84-8 二苯醚 | CAS号39515-51-0 间苯氧基苯甲醛 | CAS号3586-15-0 3-苯氧基苯甲酰氯 | CAS号133639-11-9 (2,5-dioxopyrro... | CAS号131141-93-0 N-[(3-phenoxyph... | CAS号99-06-9 3-羟基苯甲酸 | CAS号108-95-2 苯酚 | CAS号13826-35-2 3-苯氧基苄醇 | CAS号206761-84-4 3-苯氧基苯甲酰肼 | CAS号73258-84-1 3-phenoxybenzamide3-羟基苯甲酸乙酯置于copper(L) Iodide,N,N-二甲基甘氨酸,水,Caesium Carbonate,Sodium Hydroxide体系中,用 四氢呋喃,1,4-二氧六环,乙醇,N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 3-苯氧基苯甲酸
参考文献:对 Sirt 的芳氧基苯甲酰胺衍生物虚拟筛选命中的 Hit-To-Lead 优化
标题:对 Sirt 的芳氧基苯甲酰胺衍生物虚拟筛选命中的 Hit-To-Lead 优化
摘要:Sirtuins (Sirts) 是一类烟酰胺腺嘌呤二核苷酸 (Nad +) 依赖性蛋白组蛋白脱乙酰酶 (Hdac),从细菌到哺乳动物都进化保守.这组酶使用 Nad +作为共底物催化组蛋白或非组蛋白底物中赖氨酸残基的可逆脱乙酰化.大量研究表明,Sirt 的异常酶活性与糖尿病,癌症和神经退行性疾病等多种疾病有关.之前,我们进行了基于药效团的虚拟筛选活动和芳氧基苯甲酰胺衍生物 (1) 显示 Sirt1/2 抑制作用被确定为命中化合物.在当前的研究中,探索了对命中化合物的hit-To-Lead优化以改善sirt结合和抑制.已经合成了 14 种化合物,其中 10 种是新化合物,并对其对 Sirt1-3 的抑制活性进行了体外生物学评估.通过进行结构修饰,与命中化合物相比,观测到st01,St02和st11 的选择性 Sirt1 抑制显着改善.对于st14观测到最高的 Sirt2 抑制活性,这是根据与为
DOI:10.1016/j.Bmc.2020.115961
海关参考信息
- 2905110000-甲醇
2906210000-苄醇
2912110000-甲醛
2912210000-苯甲醛 - 💡 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。
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专利信息
专利号:US-3978140-A
优先权日:1974-09-23
标题 :Process for the preparation of carbinols
发明人:LANE CLINTON FISHER; MYATT HAL LESLIE
权利人:ALDRICH BORANES INC
摘要:Organic compounds containing a carboxylic acid or carboxylic acid anhydride group are reduced when contacted with an alkali metal borohydride and a boron trihalide in a liquid medium in which diborane is soluble in the form of a labile borane adduct. Hydrolysis of the reaction mixture then provides a useful synthesis of the corresponding carbinols. n The alkali metal borohydride-boron trihalide reagent may either be preformed and reacted subsequently with an organic compound containing a carboxylic acid or anhydride group, or the alkali metal borohydride-boron trihalide reagent may be produced in the presence of an organic compound containing a carboxylic acid or anhydride group. This development makes it possible to synthesize a wide variety of carbinols which are valuable and useful intermediates in organic synthesis.
专利号:US-6441246-B1
优先权日:1998-08-27
标题:Catalytic synthesis of aldehydes by direct hydrogenation of carboxylic acids
发明人:YAMAMOTO AKIO; NAGAYAMA KAZUHIRO
权利人:JAPAN SCIENCE & TECH CORP
摘要:A process which makes it possible to prepare aldehydes under mild reaction conditions with a high efficiency through the reduction of carboxylic acids with molecular hydrogen. Specifically, a process of reducing an organic carboxylic acid with molecular hydrogen in the presence of a catalyst into an aldehyde corresponding to the acid, characterized by conducting the reduction in the presence of a dehydrating agent such as a carboxylic anhydride.
专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-2009215080-A1
优先权日:2005-10-13
标题:Methods for identification of inhibitors of enzyme activity
发明人:SINHA SUKANTO; CHILCOTE TAMIE JO
权利人:ACTIVESITE PHARMACEUTICALS
摘要:The invention discloses compositions and methods of synthesis to create novel ligands and drugs and identifying such compounds as inhibitors of enzyme targets for use in the treatment of clinical disorders, including cancer, infectious diseases, parasitic infestations, neurological disorders, reproductive disorders, inflammatory disorders, circulatory disorders, and metabolic disorders.
专利号:US-8273403-B2
优先权日:2002-05-10
标题 :Generation of surface coating diversity
发明人:BARDEN MICHAEL C; KAMBOURIS PETER A
权利人:BARDEN MICHAEL C; KAMBOURIS PETER A; BIO LAYER PTY LTD
摘要:This invention relates to a surface discovery system and high-throughput combinatorial synthesis methods for generating large numbers of diverse surface coatings on solid substrates. The system is built upon a synthon which comprises at least three elements: a chemical backbone coating on the solid substrate that comprises a copolymer (B) of at least one passive constituent (P) and at least one active constituent (A); a spacer unit (S) separating the backbone from a functional group; and a functional group (F). The methods comprise the following steps: 1) selecting a plurality of synthons so that each synthon has at least two points of diversity selected from P, A, S and F; 2) applying copolymer B onto a substrate; and 3) attaching a combination of S and F to constituent A of copolymer B. Steps 2) and 3) are performed such that different synthons are generated on localized regions of the substrate.
专利号:WO-2006079916-A1
优先权日:2005-01-26
标 题 :Thieno [2,3-d] pyrimidine compounds as inhibitors of adp-mediated platelets aggregation
发明人:ENNIS MICHAEL DALTON; KORTUM STEVEN WADE; RAHMAN HAYAT; SCHWEITZER BARBARA ANN; TENBRINK RUTH ELIZABETH
权利人:PHARMACIA & UPJOHN CO LLC; ENNIS MICHAEL DALTON; KORTUM STEVEN WADE; RAHMAN HAYAT; SCHWEITZER BARBARA ANN; TENBRINK RUTH ELIZABETH
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I): wherein A1, A2, A3, A4, A5, A6, A7, A8, X4, X6, R2, R4, R5, and R6 are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.