共查询到15条相似文献,搜索用时 15 毫秒
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D. D. Rajadhyaksha D. W. Rangnekar 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》1986,36(7):300-304
Synthesis of pyrazolo[4′,3′ :-5,6′pyrido]1,2-a benzimidazoles was achieved by the condensation of 1-chloro-2-formyl-3-methyl pyrido[1,2-a]benzimidazole-4-carbonitrile and 1-chloro-3-methyl pyrido[1,2-a]benzimidazole-2,4-dicarbonitrile with hydrazine hydrate and phenyl hydrazine. The fluorescence properties of the resulting compounds were studied. Some of the compounds when applied on polyester fibres as fluorescent brighteners gave excellent results. 相似文献
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《Journal of Sulfur Chemistry》2013,34(6):595-603
Reaction of 5-(4-chlorophenyl)-2-thioxo-2,3-dihydro-1H-indeno[2',1':5,6] pyrido[2,3-d]pyrimidine-4,6-dione with hydrazonoyl chlorides gave 1,2,4-triazolo[4,3-a]pyrimidine derivatives regioselectively in good yields. The structures of the newly synthesized compounds are established on the basis of chemical and spectroscopic evidence as well as their synthesis by alternative methods. 相似文献
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A New Class of 1‐Aryl‐5,6‐dihydropyrrolo[2,1‐a]isoquinoline Derivatives as Reversers of P‐Glycoprotein‐Mediated Multidrug Resistance in Tumor Cells 下载免费PDF全文
Alisa A. Nevskaya Maria D. Matveeva Prof. Tatiana N. Borisova Dr. Mauro Niso Prof. Nicola A. Colabufo Dr. Angelina Boccarelli Dr. Rosa Purgatorio Dr. Modesto de Candia Prof. Saverio Cellamare Prof. Leonid G. Voskressensky Prof. Cosimo D. Altomare 《ChemMedChem》2018,13(15):1588-1596
A number of aza‐heterocyclic compounds, which share the 5,6‐dihydropyrrolo[2,1‐a]isoquinoline (DHPIQ) scaffold with members of the lamellarin alkaloid family, were synthesized and evaluated for their ability to reverse in vitro multidrug resistance in cancer cells through inhibition of P‐glycoprotein (P‐gp) and/or multidrug‐resistance‐associated protein 1. Most of the investigated DHPIQ compounds proved to be selective P‐gp modulators, and the most potent modulator, 8,9‐diethoxy‐1‐(3,4‐diethoxyphenyl)‐3‐(furan‐2‐yl)‐5,6‐dihydropyrrolo[2,1‐a]isoquinoline‐2‐carbaldehyde, attained sub‐micromolar inhibitory potency (IC50: 0.19 μm ). Schiff bases prepared by the condensation of some 1‐aryl‐DHPIQ aldehydes with p‐aminophenol also proved to be of some interest, and one of them, 4‐((1‐(4‐fluorophenyl)‐5,6‐dihydro‐8,9‐dimethoxypyrrolo[2,1‐a]isoquinolin‐2‐yl)methyleneamino)phenol, had an IC50 value of 1.01 μm . In drug combination assays in multidrug‐resistant cells, some DHPIQ compounds, at nontoxic concentrations, significantly increased the cytotoxicity of doxorubicin in a concentration‐dependent manner. Studies of structure–activity relationships and investigation of the chemical stability of Schiff bases provided physicochemical information useful for molecular optimization of lamellarin‐like cytotoxic drugs active toward chemoresistant tumors as well as nontoxic reversers of P‐gp‐mediated multidrug resistance in tumor cells. 相似文献
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苯并咪唑[2,1-a]并异喹啉衍生物广泛应用于生物医药、导电材料以及高分子等领域。开发其绿色的合成新方法具有重要的意义。在室温下以N-丙烯酰胺结构为自由基受体,1,3-二氧戊烷为自由基来源,荧光素为催化剂,可见光驱动下经历自由基加成/环化反应历程制备了苯并咪唑[2,1-a]并异喹啉骨架结构。在最优反应条件下,以48%~78%收率合成了11种具有不同取代基团的苯并咪唑[2,1-a]并异喹啉衍生物,采用1H NMR、13C NMR对终产物进行了结构鉴定。 相似文献
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以吡唑并[1,5-a]吡啶-2-甲醛和N-甲酰基哌嗪为原料,经过还原胺化反应、水解反应、N-烷基化反应,合成了2-[4-(4-氟苄基)哌嗪-1-基甲基]吡唑并[1,5-a]吡啶,总收率29.5%,用1HNMR、19FNMR、ESI-MS对中间体及目标化合物进行了结构表征,并通过体外受体结合实验,测定目标化合物对多巴胺D4受体的亲和常数为1.2nmol/L,对D2、D3受体的亲和常数分别为3 900、1 890 nmol/L,显示对多巴胺D4受体具有较高的亲和性与选择性,是一种潜在的多巴胺D4受体配基。 相似文献
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Yu Zhou Xun Ji Guannan Liu Dengyou Zhang Linxiang Zhao Hualiang Jiang Hong Liu 《Advanced Synthesis \u0026amp; Catalysis》2010,352(10):1711-1717
An efficient and convenient method was developed for the one‐pot construction of the complex polycyclic heterocycles pyrrolo[1,2‐a:2′,1′‐c]‐/pyrido[2,1‐c]pyrrolo[1,2‐a]quinoxalinones from two simple starting materials via a gold(I)‐catalyzed domino reaction. This strategy presents an atom economical and environmentally friendly transformation, in which two new C N bonds and one new C C bond are formed in a one‐pot reaction process. 相似文献
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《Journal of Sulfur Chemistry》2013,34(5):539-547
A series of new 2-arylthio-3-ethoxycarbonyl-6-arylimidazo[2,1-b]thiazoles (4a–4h) and 2-arenesulfonyl-3-ethoxycarbonyl-6-arylimidazo[2,1-b]thiazoles (5a–5h) have been prepared and characterized by analytical and spectral methods. The title compounds 4a–4h and 5a–5h were obtained by the reaction of 2-amino-4-ethoxycarbonyl-5-arylthiothiazoles (2a and 2b)/2-amino-4-ethoxycarbonyl-5-arenesulphonyl-thiazoles (3a and 3b) with various phenacyl bromides in anhydrous ethanol. These newly synthesized compounds (4a–4h and 5a–5h) were screened for their antibacterial activity against Gram-negative bacterium Escherichia coli, Gram-positive bacterium Staphylococcus aureus, and antifungal properties against Aspergillus niger and Candida albicans. 相似文献
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Dr. Javier García-Marín Mercedes Griera Dr. Ramón Alajarín Prof. Manuel Rodríguez-Puyol Dr. Diego Rodríguez-Puyol Prof. Juan J. Vaquero 《ChemMedChem》2021,16(18):2895-2906
Protein tyrosine phosphatase 1B (PTP1B) is a very promising target for the treatment of metabolic disorders such as type II diabetes mellitus. Although it was validated as a promising target for this disease more than 30 years ago, as yet there is no drug in advanced clinical trials, and its biochemical mechanism and functions are still being studied. In the present study, based on our experience generating PTP1B inhibitors, we have developed and implemented a scaffold-hopping approach to vary the pyrrole ring of the pyrrolo[1,2-a]quinoxaline core, supported by extensive computational techniques aimed to explain the molecular interaction with PTP1B. Using a combination of docking, molecular dynamics and end-point free-energy calculations, we have rationally designed a hypothesis for new PTP1B inhibitors, supporting their recognition mechanism at a molecular level. After the design phase, we were able to easily synthesize proposed candidates and their evaluation against PTP1B was found to be in good concordance with our predictions. Moreover, the best candidates exhibited glucose uptake increments in cellulo model, thus confirming their utility for PTP1B inhibition and validating this approach for inhibitors design and molecules thus obtained. 相似文献
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Lili An Junfeng Tong Chunyan Yang Xu Zhao Xunchang Wang Yangjun Xia 《Polymer International》2020,69(2):192-205
Three donor‐π‐acceptor (D‐π‐A) type alternating conjugated polymers, namely PIDTT‐DTNT‐C16, PIDTT‐DTNT‐HD and PIDTT‐DTNT‐OD bearing the same backbone of indacenodithieno[3,2‐b]thiophene (IDTT) as the D unit and naphtho[1,2‐c:5,6‐c′]bis[1,2,5]thiadiazole (NT) as the A moiety but with different flexible side chain (n‐hexadecyl (C16), 2‐hexyldecyl (HD) and 2‐octyldodecyl (OD)) substituted thiophene employed as π‐bridges, were synthesized and characterized. The effects of the side chain on absorption, photostability, energy levels, aggregation, backbone conformation, morphology and photovoltaic properties were systematically investigated. Because moderate D and strong A units were selected to construct the polymer backbone, a medium optical bandgap (ca. 1.66 eV) and low‐lying highest occupied molecular orbital energy level (EHOMO ≈ ?5.36 V), thus resulting in a relatively higher open‐circuit voltage (VOC) of 0.80–0.83 V, were achieved. It was found that the side chain gave rise to an insignificant impact on absorption, aggregation and photostability in chlorobenzene solution and energy levels but a non‐negligible influence on absorption, photostability and aggregation behavior in the film state. It was found that PIDTT‐DTNT‐C16 with the densest and most ordered packing structure exhibited the best photostability. Inverted bulk heterojunction polymer solar cells based on PIDTT‐DTNT‐HD:PC61BM ([6,6]‐phenyl‐C61‐butyric acid methyl ester) showed at least a 1.5‐fold increase in power conversion efficiency, chiefly originating from its slightly improved absorption, more balanced μh/μe ratio and favorable morphology of the active layer as a result of incorporating branched HD side chains into the IDTT‐alt‐DTNT backbone. © 2019 Society of Chemical Industry 相似文献
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GluN2B‐Selective N‐Methyl‐d‐aspartate (NMDA) Receptor Antagonists Derived from 3‐Benzazepines: Synthesis and Pharmacological Evaluation of Benzo[7]annulen‐7‐amines 下载免费PDF全文
Dr. Andre Benner Alessandro Bonifazi Chikako Shirataki Louisa Temme Dr. Dirk Schepmann Prof. Wilma Quaglia Prof. Osami Shoji Prof. Yoshihito Watanabe Dr. Constantin Daniliuc Prof. Dr. Bernhard Wünsch 《ChemMedChem》2014,9(4):741-751
Given their high neuroprotective potential, ligands that block GluN2B‐containing N‐methyl‐D ‐aspartate (NMDA) receptors by interacting with the ifenprodil binding site located on the GluN2B subunit are of great interest for the treatment of various neuronal disorders. In this study, a novel class of GluN2B‐selective NMDA receptor antagonists with the benzo[7]annulene scaffold was prepared and pharmacologically evaluated. The key intermediate, N‐(2‐methoxy‐5‐oxo‐6,7,8,9‐tetrahydro‐5H‐benzo[7]annulen‐7‐yl)acetamide ( 11 ), was obtained by cyclization of 3‐acetamido‐5‐(3‐methoxyphenyl)pentanoic acid ( 10 b ). The final reaction steps comprise hydrolysis of the amide, reduction of the ketone, and reductive alkylation, leading to cis‐ and trans‐configured 7‐(ω‐phenylalkylamino)benzo[7]annulen‐5‐ols. High GluN2B affinity was observed with cis‐configured γ‐amino alcohols substituted with a 3‐phenylpropyl moiety at the amino group. Removal of the benzylic hydroxy moiety led to the most potent GluN2B antagonists of this series: 2‐methoxy‐N‐(3‐phenylpropyl)‐6,7,8,9‐tetrahydro‐5H‐benzo[7]annulen‐7‐amine ( 20 a , Ki=10 nM ) and 2‐methoxy‐N‐methyl‐N‐(3‐phenylpropyl)‐6,7,8,9‐tetrahydro‐5H‐benzo[7]annulen‐7‐amine ( 23 a , Ki=7.9 nM ). The selectivity over related receptors (phencyclidine binding site of the NMDA receptor, σ1 and σ2 receptors) was recorded. In a functional assay measuring the cytoprotective activity of the benzo[7]annulenamines, all tested compounds showed potent NMDA receptor antagonistic activity. Cytotoxicity induced via GluN2A subunit‐containing NMDA receptors was not inhibited by the new ligands. 相似文献
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Nancy S. Mills James L. Malandra Antoinette Hensen John A. Lowery 《Polycyclic Aromatic Compounds》2013,33(4):239-247
Synthesis of diindeno[1,2,3,4-defg: 1′,2′,3′,4′-mnop]chrysene (1), a portion of the C60 surface, was attempted through oxidative cyclization of tetrabenzo[5.5]fulvalene (2), dibenzo[gp]chrysene (3), and diphenylmethylidenefluorene (4) by SbF5/SO2CIF. Compounds 2 and 3 were oxidized to dications which then underwent a single cyclization to give precursors to 1. Compound 4 underwent two oxidative cyclizations to give a precursor to 1. AM1 calculations of the possible products from cyclization were consistent with preferential formation of the cyclized product with the lower ΔHf. Oxidative cyclization may offer a one-pot synthetic alternative for the preparation of unusual polycyclic aromatic hydrocarbons. 相似文献
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The direct hydroxylation of toluene with nitrous oxide to cresol has been studied on two different H[Al]ZSM-5 zeolites with an Si/Al ratio of around 25 and different crystal sizes (30-70 nm and 1-3 m). The samples were activated by calcination and characterized by X-ray diffraction, temperature programmed desorption of ammonia, adsorption of nitrogen and transmission electron microscopy. For the two different crystal sizes, different macroscopic cresol yields and time on stream behaviours are observed. The sample having larger crystals shows a decrease in toluene conversion with increasing reaction temperature. For the smaller crystals an increase in toluene conversion, selectivity to cresol and amount of para-cresol in the cresol fraction with increasing reaction temperature is observed. The para-cresol selectivity is lower on the sample with the longer diffusion path. The findings are explained by product diffusion limitation caused by high reactivity and strong adsorption of the polar product cresol on H[Al]ZSM-5, resulting in a rapid deactivation of the larger crystals. 相似文献