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该文重点讨论了异吲哚啉及异吲哚啉酮颜料的品种,分子结构,特性与应用;颜料的合成工艺,颜料化和相关中间体.该类颜料以黄色品种为主,由于存在分子间及分子内氢键、并构成立体的网状堆砌,具有优异的牢度性能和重要用途. 相似文献
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该文重点讨论了异吲哚啉及异吲哚啉酮颜料的品种,分子结构,特性与应用;颜料的合成工艺,颜料化和相关中间体.该类颜料以黄色品种为主,由于存在分子间及分子内氢键、并构成立体的网状堆砌,具有优异的牢度性能和重要用途. 相似文献
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以苯胺类衍生物为起始原料,先经Sandmeyer合成得到靛红类衍生物,再经水合肼还原得到系列吲哚-2-酮类衍生物:7-氯吲哚-2-酮、5-氯吲哚-2-酮、5-甲基吲哚-2-酮和5-溴吲哚-2-酮,产率分别为52.1%、49.8%、59.3%和65.2%。 相似文献
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通过N-取代-2-吲哚酮与异氰酸酯反应,以80%-88%的收率方便高效地合成了5种新的N-取代-2-吲哚酮-3-酰胺类化合物。所有化合物均通过核磁共振谱(~1H NMR和~(13)C NMR)及高分辨质谱(HRMS)进行了结构表征。 相似文献
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以3-氟-4-硝基苯甲醚为起始原料,依次通过与丙二酸二乙酯取代、脱羧、酯化、关环反应得到目标产物5-甲氧基吲哚-2-酮,并对其合成条件进行优化,整体路线反应条件温和,适合放大,得到的产品纯度达99%,总收率达44.0%,对其结构进行了核磁表征.希望本文对同行有一些借鉴作用. 相似文献
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Mach UR Hackling AE Perachon S Ferry S Wermuth CG Schwartz JC Sokoloff P Stark H 《Chembiochem : a European journal of chemical biology》2004,5(4):508-518
Based on N-alkylated 1,2,3,4-tetrahydroisoquinoline derivatives, which are structurally related to the partial agonist BP 897, a series of novel, selective dopamine D3 receptor antagonists has been synthesised. Derivatisation included changes in the arylamide moiety and the tetrahydroisoquinoline substructure leading to compounds with markedly improved selectivities and affinities in the low nanomolar concentration range. From the 55 structures presented here, (E)-3-(4-iodophenyl)-N-(4-(1,2,3,4-tetrahydroisoquinolin-2-yl)butyl)acrylamide (51) has high affinity (Ki(hD3)=12 nM) and a 123-fold preference for the D3 receptor relative to the D2 receptor subtype. Its pharmacological profile offers the prospect of a novel radioligand as a tool for various dopamine D3-receptor-related in vitro and in vivo investigations. 相似文献
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Pellicciari R Filosa R Fulco MC Marinozzi M Macchiarulo A Novak C Natalini B Hermit MB Nielsen S Sager TN Stensbøl TB Thomsen C 《ChemMedChem》2006,1(3):358-365
The first series of 2'-substituted 2-(3'-carboxybicyclo[1.1.1]pentyl)glycine derivatives, (2R)- and (2S)-(2',2'-dichloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (10) and (11), and 2-(2'-chloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (12) were synthesized and evaluated as mGluR ligands. Compounds 11 and 12 were shown to be competitive group I mGluR antagonists. These results are also discussed in light of docking studies with both the active (closed) and inactive (open) conformations of mGluR1. 相似文献
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Yu XM Ramiandrasoa F Guetzoyan L Pradines B Quintino E Gadelle D Forterre P Cresteil T Mahy JP Pethe S 《ChemMedChem》2012,7(4):587-605
New N‐alkylaminoacridine derivatives attached to nitrogen heterocycles were synthesized, and their antimalarial potency was examined. They were tested in vitro against the growth of Plasmodium falciparum, including chloroquine (CQ)‐susceptible and CQ‐resistant strains. This biological evaluation has shown that the presence of a heterocyclic ring significantly increases the activity against P. falciparum. The best compound shows a nanomolar IC50 value toward parasite proliferation on both CQ‐susceptible and CQ‐resistant strains. The antimalarial activity of these new acridine derivatives can be explained by the two mechanisms studied in this work. First, we showed the capacity of these compounds to inhibit heme biocrystallization, a detoxification process specific to the parasite and essential for its survival. Second, in our search for alternative targets, we evaluated the in vitro inhibitory activity of these compounds toward Sulfolobus shibatae topoisomerase VI‐mediated DNA relaxation. The preliminary results obtained reveal that all tested compounds are potent DNA intercalators, and significantly inhibit the activity of S. shibatae topoisomerase VI at concentrations ranging between 2.0 and 2.5 μM . 相似文献
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双端8-羟基喹啉配体的合成与表征 总被引:2,自引:0,他引:2
设计了以8-羟基喹啉为原料,经过氯甲基化后分别与哌嗪、十二胺、癸二醇反应,合成了3种端基为8-羟基喹啉的双端配体,即N,N'-双(8-羟基喹啉基5-亚甲基)哌嗪、N,N-双(8-羟基喹啉基5-亚甲基)十二胺、O,O'-双(8-羟基喹啉基-5-亚甲氧基)癸烷.通过元素分析、核磁共振谱对3种化合物的组成和结构进行了表征. 相似文献
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为筛选到活性更好的抗肿瘤PI3K抑制剂,以2,4-二羟基吡啶为原料,经氯化后和吗啡啉反应、碘代、Sonogashira偶联、脱保护基与叠氮化反应得到三氮唑中间体8~13,最后经Suzuki反应,偶联上芳基得到2-芳基-4-吗啉-6-三氮唑基嘧啶14~27,其结构均经1HNMR和LC-MS确证。用MTT法评价了化合物14~27对PI3K高表达的人卵巢细胞A2780增殖的抑制活性,其中,在化合物测试浓度为10μmol/L时,14和25的抑制活性均高于正在临床实验的阳性对照药物GDC-0941和BEZ-235,抑制率分别达到76.7%与77.2%。这两个化合物在小鼠体内代谢良好,其中化合物25更为优异t1/2为3.2 h,药时曲线下面积AUC0-∞为34 193(ng·h)/mL。 相似文献
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Hendrix JA Shimshock SJ Shutske GM Tomer JD Kapples KJ Palermo MG Corbett TJ Vargas HM Kafka S Brooks KM Laws-Ricker L Lee DK de Lannoy I Bordeleau M Rizkalla G Owolabi J Kamboj RK 《Chembiochem : a European journal of chemical biology》2002,3(10):999-1009
A new class of potent dopamine D(4) antagonists was discovered with selectivity over dopamine D(2) and the alpha-1 adrenoceptor. The lead compound was discovered by screening our compound collection. The structure-activity relationships of substituted isoindoline rings and the chirality about the hydroxymethyl side chain were explored. The isoindoline analogues showed modest differences in potency and selectivity. The S enantiomer proved to be the more potent enantiomer at the D(4) receptor. Several analogues with greater than 100-fold selectivity for D(4) over D(2) and the alpha-1 adrenoreceptor were discovered. Several selective analogues were active in vivo upon oral or intraperitoneal administration. A chiral synthesis starting from either D- or L-O-benzylserine is also described. 相似文献