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1.
Victor Israel Cohen 《Journal of heterocyclic chemistry》1979,16(1):13-16
A new one-step facile method for the synthesis of some benzimidazole, benzoxazole and benzothiazole derivatives is described. The method involves the action of aromatic and heterocyclic selenoamides on some o-phenylenediamine, o-aminophenol and o-aminothiophenol and their derivatives. 相似文献
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Novel azo linked substituted benzimidazole, benzoxazole, and benzothiazole were synthesized by diazo coupling and characterized by 1H NMR, elemental analysis, FTIR and UV–vis spectroscopy. The newly synthesized compounds were evaluated for invitro antibacterial activity against Staphylococcus aureus and Escherichia Coli strains by Resazurin microtiter assay method (REMA). The minimum inhibitory concentration (MIC in μg/mL) were used to express the antibacterial activities. The azo linked compounds exhibited good to moderate or high antibacterial activities in vitro. Computational studies were performed to correlate HOMO-LUMO gap with antibacterial activity. The comparative molecular docking studies revealed better insights into binding mechanisms. 相似文献
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The optimized structures of all isomers of HBI, HBO, HBT, HPyBI, HPyBO, and HPyBT compounds were obtained using the potential
energy surface method at the B3LYP/6-311++G(d,p) level of theory. Four isomers and three transition states of their transformations
for each compound of HBO, HBT, HPyBO, and HPyBT and two isomers and one transition state for each HBI and HPyBI compounds
were found. Energetics, thermodynamic properties, rate constants, and equilibrium constants of their transformations were
determined.
Electronic supplementary material The online version of this article (doi:) contains supplementary material, which is available to authorized users. 相似文献
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A series of substituted benzimidazoles, benzothiazoles, and benzoxazoles was synthesized by combining 1,2-phenylenediamine, 2-aminothiophenol, or 2-aminophenol with aryl, heteroaryl, aliphatic, α,β-unsaturated aldehydes in the presence of nano ceria (CeO2) as an efficient heterogeneous catalyst. 相似文献
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In a previous hit-to-lead research program targeting anticancer agents, two promising lead compounds, 1a and 1b, were found. However, the poor solubility of 1a and 1b made difficult further in vivo studies. To solve this problem, a lead optimization was conducted through introducing N-methyl-piperazine groups at the 2-position and 6-position. To our delight, the optimized analogue 1d showed comparable antiproliferative activity in vitro with better solubility, compared with 1a. Based on this result, the replacement of the benzothiazole scaffold with benzimidazole and benzoxazole moieties afforded 1f and 1g, whose activities were fundamentally retained. In the preliminary in vitro biological evaluation, the immunofluorescence staining of HCT116 cells indicated that 1d, 1f and 1g led to cytosolic vacuolization which was not induced by 1a at low micromolecular concentrations. These results suggest that these optimized compounds might potentially constitute a novel class of anticancer agents, which merit further studies. 相似文献
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Heraclio López-Ruiz Horacio Briseño-OrtegaSusana Rojas-Lima Rosa SantillanNorberto Farfán 《Tetrahedron letters》2011,52(33):4308-4312
A novel, one-pot, phenylboronic acid catalyzed, cyanide promoted synthesis of 2-(2-hydroxyphenyl)benzoxazoles from salicylaldehydes and o-aminophenols is described. The synthesis is characterized by mild conditions, short reaction times, and simple workup of crystalline, high purity products. 相似文献
11.
Aliphatic selenonesters react with o-phenylenediamine, o-aminophenol and o-aminothiophenol and their derivatives to form benzimidazole, benzoxazole and benzothiazole derivatives, respectively. The mass and nmr spectra of the mentioned compounds were studied. 相似文献
12.
Hiba Kottayil Shaibuna Machingal Sherly mole Parackal B. Shebitha Alungal M. Letcy V. Theresa Avudaiappan Govindan Sreekumar Krishnapillai 《Journal of heterocyclic chemistry》2020,57(9):3310-3317
A new polyamine was prepared by the ring opening polymerization of epichlorohydrin and properly characterized. The catalytic property of the prepared polymer was assessed by synthesizing 2-aryl-substituted benzimidazole and benzoxazole derivatives by the conjugation of o-phenylenediamine/o-aminophenol with various aromatic aldehydes in the presence of atmospheric oxygen. Significant attributes of the present synthesis include short reaction time, good to excellent yield, high purity, easy reusability, and room temperature reaction. The reaction was carried out in the absence of any metal catalyst and other cooxidants. 相似文献
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Srinivasulu Ramineni Ravi Kumar Kannasani V.V. Satyanarayana Peruri 《Green Chemistry Letters and Reviews》2014,7(1):85-89
A simple and efficient method has been developed for the synthesis of benzoxazoles from 2-aminophenol and substituted aldehydes in the presence of a catalytic amount of zinc triflate in ethanol solvent at reflux temperature. 相似文献
15.
利用人工受体与适当底物间的分子识别以建立仿生模型的研究已成为生物有机化学的前沿领域之一。作为一类新型的人工受体,分子裂缝近年来在分子识别、生物传感、外消旋体的拆分、分子器件等领域引起越来越多的关注[1-3]。胆甾因其具有刚性的凹面结构和固有的手性,是构筑钳形人工 相似文献
16.
Tuba GÜNG
R 《Turkish Journal of Chemistry》2021,45(1):219
A series of novel imidazo[1,2- a ]pyrimidine containing tri/tetrasubstituted imidazole derivatives (1-10) has been synthesized via sequential two-step, one-pot, multicomponent reaction using imidazo[1,2- a ]pyrimidine-2-carbaldehyde, benzil, primary amines, and ammonium acetate catalyzed by p -toluenesulfonic acid under microwave-assisted conditions. The results showed that target compounds can be obtained from a wide range of primary amines bearing different functional groups with moderate to good yields (46%-80%) under optimum reaction conditions. This method provides a green protocol for imidazo[1,2- a ]pyrimidine containing tri/tetrasubstituted imidazole derivatives due to ethyl alcohol as a green solvent, microwave irradiation as a greener heating method and one-pot multicomponent reaction as a green technique. The synthesized compounds have been elucidated using various spectroscopic tools such as FT-IR, 1H NMR, 13 C NMR, and MS. 相似文献
17.
《Arabian Journal of Chemistry》2022,15(12):104366
We report microwave synthesis of seven unique pyrimidine anchored derivatives (1–7) incorporating multifunctional amino derivatives along with their in vitro anticancer activity and their activity against COVID-19 in silico. 1–7 were characterized by different analytical and spectroscopic techniques. Cytotoxic activity of 1–7 was tested against HCT116 and MCF7 cell lines, whereby 6 exhibited highest anticancer activity on HCT116 and MCF7 with EC50 values of 89.24 ± 1.36 µM and 89.37 ± 1.17 µM, respectively.Molecular docking was performed for derivatives (1–7) on main protease for SARS-CoV-2 (PDB ID: 6LU7). Results revealed that most of the derivatives had superior or equivalent affinity for the 3CLpro, as determined by docking and binding energy scores. 6 topped the rest with highest binding energy score of ?8.12 kcal/mol with inhibition constant reported as 1.11 µM. ADME, drug-likeness, and pharmacokinetics properties of 1–7 were tested using Swiss ADME tool. Toxicity analysis was done with pkCSM online server.All derivatives showed high GI absorption. Except 1 and 3, all derivatives showed blood brain barrier permeability. Most derivatives showed negative logKp values suggesting derivatives are less skin permeable and bioavailability score of all derivatives was 0.55. The toxicity analysis demonstrated that all derivatives have no skin sensitization properties. 6 and 7 showed maximum tolerated dose (Human) values of ?0.03 and ?0.018, respectively and absence of AMES toxicity. 相似文献
18.
Chen Hui Li Hua Yu Qiu Cai Hong Xu 《中国化学快报》2007,18(12):1436-1438
Bis-silicon-bridged stilbene derivatives were synthesized in a modified procedure that combined the preparation of bis[2- (silyl)phenyl]acetylene and its intramolecular reductive cyclization in one pot.The results indicated that the one pot approach produced target products in a comparable yield to that of the two-step method reported previously. 相似文献
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A straightforward, efficient and more sustainable catalyst-free method has been developed for the synthesis of quinoxaline, benzoxazole, and benzimidazole ring system in glycerol to achieve yields that were comparable to or better than, those in conventional media. It is noteworthy that the reaction was exclusively carried out in glycerol-water system, rendering the methodology highly valuable from both environment and economic points of view. 相似文献
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Developed a convenient and mild one pot synthesis of cyclopentenone derivatives using 1-acetyl-1-cyclohexene and wide range of aldehydes. Aromatic and heterocyclic aldehydes with electron donating and withdrawing groups were conveniently converted to the corresponding cyclopentenone derivatives. 相似文献