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1.
The present paper describes the synthesis of 5‐azido‐6‐ketones (14) and 6‐hydroxy‐5‐ketone (20) from Hajos Wiechert ketone as chiral building blocks for cephalostatin analogues. The synthesis of symmetric cephalostatin analogue from 6‐hydroxy‐5‐ketone has also been reported. The characterization of the each synthesized compounds was carried out by IR, 1H‐NMR, 13C‐NMR and High resolution Mass Spectrometry. 相似文献
2.
The base catalyzed intramolecular nucleophilic cyclization of 1‐(2‐haloaroyl)‐3‐aryl thioureas ( 1a‐i ), in the presence of DMF afforded the 1‐aryl‐2‐thioxo‐2,3‐dihydro‐1H‐quinazolin‐4‐ones ( 2a‐i ). The structures were confirmed by spectroscopic data, elemental analyses and in case of the 2c by single crystal X‐ray diffraction data. The mechanistic studies support an intramolecular nucleophilic substitution (SNAr mechanism) rather than intramolecular aromatic substitution (SRN1 mechanism). 相似文献
3.
Synthesis and antimicrobial activity of some novel 2-(substituted fluorobenzoylimino)-3-(substituted fluorophenyl)-4-methyl-1,3-thiazolines 总被引:1,自引:0,他引:1
The synthesis of several 2-(substituted fluorobenzoylimino)-3-(substituted fluorophenyl)-4-methyl-1,3-thiazolines (2a-t) was carried out by base-catalyzed cyclization of corresponding 1-(fluorobenzoyl)-3-(fluorophenyl)thioureas (1a-t) with 2-bromoacetone in aqueous medium. The structures of the synthesized compounds were confirmed by spectral and elemental analysis. All synthesized compounds were evaluated for in vitro antibacterial activity using Gram-positive bacteria (Staphylococcus aureus, Bacillus subtilis) and Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa). The minimum inhibitory concentration (MIC) was determined for the most active compounds. In vitro antifungal activity was also determined against the five fungal species (Rhizopus oryzae, Fusarium oxysporum, Aspergillus terreus, A. niger and A. fumigatus). 相似文献
4.
A. Venkateswara Rao Uzma K. H. Bangi Sunetra L. Dhere Hiroaki Imai Hiroshi Hirashima 《Journal of Sol-Gel Science and Technology》2011,57(1):95-100
The effect of iron acetylacetonate on the physico-chemical properties of waterglass based silica aerogels by ambient pressure
drying has been investigated. Doping the gels with iron acetylacetonat (FeAA) facilitates in the diminution of the density
of the aerogels. The well established silica network provides effective confinement of FeAA nanoparticles which resists the
collapse of silica network during ambient pressure drying. Therefore, in the present paper, the effects of FeAA on the physico-chemical
properties of the aerogels have been studied by varying the FeAA:Na2SiO3 molar ratio from 3 × 10−4 to 6 × 10−4. The aerogels were prepared via ambient pressure drying and characterized by the bulk density, thermal conductivity and water
contact angle. The aerogel’s surface morphology, elemental analysis and pore structure were characterized by means of EDAX
and FTIR, TEM and N2 adsorption- desorption analyzer. The high temperature hydrophobicity of these aerogels was checked by heating them in temperature
controlled furnace. Silica aerogels with low density ~0.050 g/cc have been obtained using the molar ratio of Na2SiO3:H2O:FeAA:Citric acid:TMCS at 1:146.67:3 × 10−4:0.54:9.46, respectively. EDAX and FTIR studies show that the iron species are entrapped in the mesoporous framework and not
took part in the bonding with silica. 相似文献
5.
Four new carbamates (RZ1–RZ4) were synthesized from different amine moieties through reported methods. The reaction was monitored using thin layer chromatography and characterization was done using m.p., fourier‐transform infrared spectroscopy (FTIR), and X‐ray diffraction (XRD) techniques. Density functional theory (DFT) studies were carried out using Gaussian 09 software to compare the theoretical and practical parameters of the synthesized compounds. Highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) were also drawn to calculate the energy difference between orbitals. In‐vitro enzyme inhibition potential against acetylcholine esterase (AChE), butyrylcholine esterase (BChE), and protease was checked through standard protocols that suggested moderate inhibition against selected enzymes. Docking studies were also carried out, which depicted that these compounds have ability to bind on the active site of AChE and BChE. 相似文献
6.
A. Parvathy Rao A. Venkateswara Rao Uzma K. H. Bangi 《Journal of Sol-Gel Science and Technology》2008,47(1):85-94
The experimental results on the preparation of low thermal conductivity and transparent ambient pressure dried silica aerogels
with the sodium silicate solution, TMCS silylating agent with methanol, isopropyl alcohol, hexane and xylene solvents, are
reported. This study is focussed on the effect of preparation conditions such as varying the number of preparation steps,
pH of the hydrosol and hydrogel ageing temperature, for the production of the low thermal conductive silica aerogels and the
results are analysed. Density, thermal conductivity, % of optical transmission and contact angle of the aerogels were measured.
The Fourier Transform Infrared Spectroscopy (FTIR) studies revealed the presence of Si–C and C–H along with the Si–O–Si and
OH bonds and their intensities strongly depend on the processing steps, pH of the hydrosol and gel ageing temperature. The
UV–Visible spectra indicated the % of optical transmission of the aerogels decreased with increasing the number of processing
steps, increase in the pH of the hydrosol from 3 to 8 and decreased for ageing temperature up to 50 °C. Further increase in
temperature >50 °C, the % of optical transmission of the aerogels increased. The TGA-DTA data showed the thermal stability
of the aerogels with respect to hydrophobicity is 325 °C. Transmission Electron Microscopy (TEM) and Scanning Electron Microscopy
(SEM) analyses revealed the nanostructure of the aerogels. The porosity of the aerogels was studied using the pore size distribution.
Silica aerogels with low density (0.051 g/cc), low thermal conductivity (0.049 W/m K), optical transmission (65%), high hydrophobicity
(159°) and resistance to humid atmosphere >1 year was obtained in the present studies. 相似文献
7.
A digraph is associated with a finite group by utilizing the power map f: G → G defined by f(x) = xkfor all x ∈ G, where k is a fixed natural number. It is denoted by γG(n, k). In this paper, the generalized quaternion and 2-groups are stud- ied. The height structure is discussed for the generalized quaternion. The necessary and sufficient conditions on a power digraph of a 2-group are determined for a 2-group to be a generalized quaternion group. Further, the classification of two generated 2-groups as abelian or non-abelian in terms of semi-regularity of the power digraphs is completed. 相似文献
8.
Hydrogen generation from weak acids: electrochemical and computational studies of a diiron hydrogenase mimic 总被引:1,自引:0,他引:1
Felton GA Vannucci AK Chen J Lockett LT Okumura N Petro BJ Zakai UI Evans DH Glass RS Lichtenberger DL 《Journal of the American Chemical Society》2007,129(41):12521-12530
Extended investigation of electrocatalytic generation of dihydrogen using [(mu-1,2-benzenedithiolato)][Fe(CO)3]2 has revealed that weak acids, such as acetic acid, can be used. The catalytic reduction producing dihydrogen occurs at approximately -2 V for several carboxylic acids and phenols resulting in overpotentials of only -0.44 to -0.71 V depending on the weak acid used. This unusual catalytic reduction occurs at a potential at which the starting material, in the absence of a proton source, does not show a reduction peak. The mechanism for this process and structures for the intermediates have been discerned by electrochemical and computational analysis. These studies reveal that the catalyst is the monoanion of the starting material and an ECEC mechanism occurs. 相似文献
9.
Glass RS Block E Lorance E Zakai UI Gruhn NE Jin J Zhang SZ 《Journal of the American Chemical Society》2006,128(39):12685-12692
The ionization energies of conformationally constrained, newly synthesized beta-disilanyl sulfides and selenides were determined by photoelectron spectroscopy. These ionization energies reflect substantial (0.53-0.75 eV) orbital destabilizations. The basis for these destabilizations was investigated by theoretical calculations, which reveal geometry-dependent interaction between sulfur or selenium lone pair orbitals and sigma-orbitals, especially Si-Si sigma-orbitals. These results presage facile redox chemistry for these compounds and significantly extend the concept of sigma-stabilization of electron-deficient centers. 相似文献
10.
Uzma Habib Amin Badshah Ulrich Flörke Rizwana Aleem Qureshi Bushra Mirza Nazar-ul-Islam Azeem Khan 《Journal of chemical crystallography》2009,39(10):730-734
Abstract The reaction of Cu(OOCCH3)2·H2O with (2,4-diamino-5-(3′,4′,5′-trimethoxybenzyl) pyrimidine (trimethoprim) in ethanolic solution at 80 °C affords the title
complex which has been characterized by elemental, IR, and NMR (1H and 13C).The crystal structure has been determined by single crystal X-ray diffraction. Compound 1 (C36H48Cu2N8O14) is triclinic, space group P-1 with a = 7.2676(4) ?, b = 11.6721(7) ?, c = 12.8279(8) ?, α = 95.839(1)°, β = 93.456(1)°, γ = 105.541(1)°, Z = 1. Two copper atoms are coordinated directly to each other as well as are held together by four bridging aceto groups.
Each copper atom is also bonded opposite the Cu–Cu vector to a trimethoprim molecule through the N(1) atom of the pyrimidine
ring. Trimethoprim acts as a monodentate ligand through the pyrimidine nitrogen N(1) atom. The complex was screened for the
activity against several bacteria, showing more activity against bacteria as compared to trimethoprim.
Graphical Abstract To enhance the activity of trimethoprim, its derivative was prepared and there bacterial activity against several bacteria
was analyzed.
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