共查询到20条相似文献,搜索用时 15 毫秒
1.
Nehad A. Abdel-Latif Nermien M. Sabry Ashraf M. Mohamed Mohamed M. Abdulla 《Monatshefte für Chemie / Chemical Monthly》2007,138(7):715-724
Summary. A series of substituted pyridine, pyrazoline, and thiopyrimidine derivatives were synthesized from 3-acetylpyridine, which
was prepared from nicotinic acid as a naturally starting material. The pharmacological screening showed that many of these
compounds have good analgesic and antiparkinsonian activities comparable to Voltarene? and Benzatropine? as reference drugs. The structure assignment of the new compounds is based on chemical and spectroscopic evidence. The detailed
synthesis, spectroscopic data, and pharmacological properties for synthesized compounds are reported. 相似文献
2.
Karema N. M. Halim Sameh A. Rizk Maher A. El-Hashash Sayed K. Ramadan 《Journal of heterocyclic chemistry》2021,58(2):636-645
Tetrahydropyrimidinone derivative was synthesized through one-pot three components condensation of 1,3-diphenylpyrazole-4-carbaldehyde with pentan-2,4-dione and urea under Biginelli reaction conditions. The corresponding chloro- and hydrazino derivatives were synthesized and utilized for the construction of some valuable N-heterocycles encompassing both pyrazole and pyrimidine cores, such as triazolopyrimidine, tetrazolopyrimidine, pyrazole, and pyrazolone derivatives through condensation with nitrogen nucleophiles and carbon electrophiles. The antiproliferative activity evaluation of the synthesized compounds against four human carcinoma cell lines namely, liver carcinoma (HepG2), breast adenocarcinoma (MCF7), prostate cancer (PC3), and colon cancer (HCT-116) cell lines revealed that some of them provided significant potency, as well as the density-functional theory (DFT) was studied. The permeability of various hydrophilic and hydrophobic synthesized compounds across both normal and cancer cells is confirmed via DFT simulation in which the much higher permeability through aquaporin channels revealed the selective cytotoxicity toward cancer cells. 相似文献
3.
Bharat B. Kashid Anil A. Ghanwat Vijay M. Khedkar Balasaheb B. Dongare Mubarak H. Shaikh Prathmesh P. Deshpande Yogesh B. Wakchaure 《Journal of heterocyclic chemistry》2019,56(3):895-908
A series of novel 2‐substituted benzimidazole and benzoxazole derivatives as a potential antimicrobial and antioxidant agent were synthesized via coupling of N‐methyl‐o‐phenylenediamine or 2‐amino‐phenol with aromatic aldehyde and acid in the presence of polyphosphoric acid as an efficient catalyst as well as solvent by conventional method in short reaction times with excellent yield. The newly synthesized benzimidazole and benzoxazole derivatives were evaluated for antimicrobial and antioxidant activity and exhibited excellent to good activities compared to the standard drugs. Furthermore, the theoretical predictions based on molecular docking against microbial DNA gyrase could provide an insight into the plausible mechanism of action and establish a link between the observed antimicrobial activity and the binding affinity shedding light on specific thermodynamic (bonded and nonbonded) interactions governing the activity. Furthermore, the synthesized compounds were analyzed for absorption, distribution, metabolism, and excretion properties and exhibited potential properties to build up as good oral drug candidates. 相似文献
4.
2-Cyanoacetohydrazide and 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene derivatives were exploited as starting materials for the syntheses of novel thienopyrimidines and triazolothienopyrimidines. The proclivity of these compounds toward one-carbon donor reagents such as carbon disulfide, phenyl isothiocyanate, and aromatic aldehydes was investigated. The structures of all synthesized compounds were ascertained by spectral and analytical data. The antimicrobial activity of the target synthesized compounds was tested against various microorganisms. 相似文献
5.
Naveen Gautam Shikha Gupta Neha Ajmera D. C. Gautam 《Journal of heterocyclic chemistry》2012,49(3):710-715
10H‐phenothiazines are synthesized via Smiles rearrangement. These prepared phenothiazines act as a base to prepare ribofuranosides by treating them with b‐D ‐ribofuranosyl‐1‐acetate‐2,3,5‐tribenzoate. 10H‐phenothiazines on refluxing with hydrogen peroxide in glacial acetic acid gave 10H‐phenothiazine‐5,5‐dioxides. The synthesized compounds were evaluated for their antioxidative properties through in vitro studies, and they are also screened for their antimicrobial activity. The structure of the synthesized compounds has been established by elemental analysis and spectroscopic data. 相似文献
6.
Ivanova Yu. B. Chizhova N. V. Khrushkova Yu. V. Rusanov A. I. Mamardashvili N. Zh. 《Russian Journal of General Chemistry》2019,89(3):459-465
2,3,7,8,12,13,17,18-Ocatbromo-5,10,15,20-tetra-(4-chloroprienyl)porphyrin and 2,3,7,8,12,13,17,18-octachloro-5,10,15,20-tetra-(4-bromophenyl)porphyrin have been synthesized. The obtained compounds have been identified by electronic absorption and 1H NMR spectroscopy as well as mass spectrometry. The complex-forming properties of the synthesized porphyrins in the zinc acetate (II)-acetonitrile system at 278–298 K have been studied. Kinetic parameters of the formation of the corresponding zinc complexes in acetonitrile have been determined.
相似文献7.
P. P Kulikov A. N. Kuskov A. V. Goryachaya A. N. Luss M. I. Shtil’man 《Polymer Science Series D》2017,10(3):263-268
Water-soluble amphiphilic polymers based on N-vinyl-2-pyrrolidone (Amph-PVP) have been synthesized. Amphiphilic diblock polymers have been obtained via a single-step technique. For the synthesized amphiphilic polymers, the critical concentrations of mycelium formation (CCM) have been determined. The structure of the polymers obtained was confirmed by IR and NMR spectroscopy. The critical concentration of micelle formation (CCM) for the synthesized polymers has been found to be in the micromolar range. The fluorescent dye 1,1′-dioctadecyl-3,3,3′,3′-tetramethylindocarbocyanine perchlorate (Dil) was chosen as a model substance for the synthesis of nanoparticles. Micellar particles were obtained via an ultrasonic technique followed by evaporation of the organic solvent (emulsion method). 相似文献
8.
9.
A series of 1,3-oxazole, 1,3-thiazole, isomeric 1,2,4-oxadiazole, 1,3,4-oxadiazole, and 1,2,3,4-tetrazole heterocycles was synthesized. All the compounds shared as a common feature the presence of a 4-hydroxyphenyl substituent. The structures of the synthesized compounds were confirmed by MS, 1H-NMR, and elemental analysis. In vitro antimicrobial activity for all the newly synthesized compounds at concentrations of 200-25 μg/mL was evaluated against Gram+ve organisms such as methicillin-resistant Staphylococcus aureus (MRSA), Gram-ve organisms such as Escherichia coli (E. coli), and the fungal strain Aspergillus niger (A. niger) by the cup plate method. Ofloxacin and ketoconazole (10 μg/mL) were used as reference standards for antibacterial and antifungal activity, respectively. Compounds 15, 16, and 20 showed notable antibacterial and antifungal activities at higher concentrations (200 μg/mL), whereas 17-19 were found to display significant antibacterial or antifungal activity (25-50 μg/mL) against the Gram+ve, Gram-ve bacteria, or fungal cells used in the present study. 相似文献
10.
Dr. Wenlong Yang Dr. Jorge H. S. K. Monteiro Prof. Ana de Bettencourt-Dias Prof. Vincent J. Catalano Prof. Wesley A. Chalifoux 《Chemistry (Weinheim an der Bergstrasse, Germany)》2019,25(6):1441-1445
This work explores the syntheses, structures, photophysical properties, and photostability of benzodipyrenes (BDPs). BDPs were synthesized through an InCl3-AgNTf2-catalyzed, four-fold alkyne benzannulation reaction. The structures of BDP 4 a and its corresponding endoperoxide product were unambiguously confirmed by X-ray crystallography. The BDPs reported here can also be recognized as peri- and cata-benzannulated pentacenes with a non-functionalized central ring. Unlike the previous reported pentacene-based polycyclic aromatic hydrocarbons, the absorbances of the BDPs were blueshifted by ca. 40 nm relative to pentacene, even after extension of π-conjugation. The newly synthesized BDP products exhibit relatively good stability with half-lives as high as 4612 min in THF. 相似文献
11.
Philipp Fruhmann Philipp Skrinjar Julia Weber Hannes Mikula Benedikt Warth Michael Sulyok Rudolf Krska Gerhard Adam Erwin Rosenberg Christian Hametner Johannes Fröhlich 《Tetrahedron》2014
The synthesis of several sulfates of trichothecene mycotoxins is presented. Deoxynivalenol (DON) and its acetylated derivatives were synthesized from 3-acetyldeoxynivalenol (3ADON) and used as substrate for sulfation in order to reach a series of five different DON-based sulfates as well as T2-toxin-3-sulfate. These substances are suspected to be formed during phase-II metabolism in plants and humans. The sulfation was performed using a sulfuryl imidazolium salt, which was synthesized prior to use. All protected intermediates and final products were characterized via NMR and will serve as reference materials for further investigations in the fields of toxicology and bioanalytics of mycotoxins. 相似文献
12.
Titus Constantinescu Petre Ionita Ion Chiorescu Gabriela Ionita 《Central European Journal of Chemistry》2003,1(4):465-476
Ten novel and stable free radicals of nitronyl-, imino-nitroxide and hydrazyl type compounds were synthesized and their physico-chemical
properties investigated. UV-Vis and ESR spectroscopic data, as well as the lipophilicities and specific hydrophobic areas
of the compounds are compiled. The reaction of these radical compounds with nitric oxide and nitrogen dioxide was also investigated.
The radicals synthesized, show selectivity in their reaction with these nitric oxides, depending on their structure (nitronyl-nitroxide
radicals react with NO, while hydrazyl radicals react with NO2). The processes are easily monitored by UV-Vis or ESR spectroscopy. 相似文献
13.
《Journal of heterocyclic chemistry》2017,54(1):268-277
As a part of ongoing studies in developing new potent antioxidant agents, N‐[4‐(aminosulfonyl)phenyl]‐2‐cyanoacetamide ( 3 ) was utilized as key intermediate for the synthesis of some new thiophene, chromene, and pyrazolotriazine pyridine derivatives. The structures of the newly synthesized compounds were confirmed by elemental analysis, IR, 1H‐NMR, and mass spectral data. Representative compounds of the synthesized products were tested and evaluated as antioxidant. Compounds 7 and 30 are promising compounds. 相似文献
14.
Nirmala S. Naik Navya S. Bhat Arpana G. Hegde Swati S. Bhat Akshay Kirasur Anilkumar Patil 《合成通讯》2018,48(5):511-523
For the application in organic electronics as well as pH meters, a series of novel 2,4,6-trisubstituted pyridines have been synthesized by the reaction of substituted aromatic aldehydes and substituted 3-acetylcoumarin with ammonium acetate. The structures of all the new compounds were characterized by IR, NMR, and GC–MS analysis. The important photo physical prerequisites for organoelectronic such as optical absorption and thermal stability were determined for the synthesized molecules. Optical properties were studied by UV–visible absorption and fluorescence spectroscopy. Optical band gaps of the 2,4,6-trisubstituted pyridines were found to be around 3.01–3.06?eV as calculated from their onset absorption edge. The pH-dependent changes in the fluorescence intensity suggest that 2,4,6-trisubstituted pyridines are useful applicants in intracellular pH meters. 相似文献
15.
Dr. Abdolhossein Miri Dr. Hakimeh Najafzadeh Dr. Majid Darroudi Dr. Mohammad Javad Miri Dr. Mohammad Amin Jadidi Kouhbanani Mina Sarani 《ChemistryOpen》2021,10(3):327-333
Iron oxide nanoparticles have attracted much attention because of their superparamagnetic properties and their potential applications in many fields such as magnetic storage devices, catalysis, sensors, superparamagnetic relaxometry (SPMR), and high-sensitivity biomolecule magnetic resonance imaging (MRI) for medical diagnosis and therapeutics. In this study, iron oxide nanoparticles (Fe2O3 NPs) have been synthesized using a taranjabin (camelthorn or persian manna) aqueous solution. The synthesized Fe2O3 NPs were identified through powder X-ray diffraction (PXRD), X-ray photoelectron spectroscopy (XPS), Fourier transform infrared spectroscopy (FT-IR), field energy scanning electron microscopy (FESEM), transmission electron microscopy (TEM), energy-dispersive spectroscopy (EDX), vibrating-sample magnetometer (VSM) and Raman technics. The results show that the nanoparticles have a hexagonal structure with 20 to 60 nm in size. The cytotoxic effect of the synthesized nanoparticles has been tested upon application against lung cancer cell (A549) lines. It was found that there is no cytotoxic activity at lower concentrations of 200 μg/mL. The ability of the synthesized nanoparticles for lead removal in wastewaters was tested. Results show that highest concentration of adsorbent (50 mg/L) has maximum removal efficiency (96.73 %). So, synthesized Fe2O3 NPs can be a good candidate to use as heavy metals cleaner from contaminated waters. 相似文献
16.
Pavel S. Gribanov Dmitry A. Loginov Dmitry A. Lypenko Artem V. Dmitriev Sergey I. Pozin Alexey E. Aleksandrov Alexey R. Tameev Igor L. Martynov Andrey Yu. Chernyadyev Sergey N. Osipov 《Molecules (Basel, Switzerland)》2021,26(24)
Three new benzothiadiazole (BTD)-containing luminophores with different configurations of aryl linkers have been prepared via Pd-catalyzed cross-coupling Suzuki and Buchwald–Hartwig reactions. Photophysical and electroluminescent properties of the compounds were investigated to estimate their potential for optoelectronic applications. All synthesized structures have sufficiently high quantum yields in film. The BTD with aryl bridged carbazole unit demonstrated the highest electrons and holes mobility in a series. OLED with light-emitting layer (EML) based on this compound exhibited the highest brightness, as well as current and luminous efficiency. The synthesized compounds are not only luminophores with a high photoluminescence quantum yield, but also active transport centers for charge carriers in EML of OLED devices. 相似文献
17.
Akira Shimada Yoichiro Ezaki Junji Inanaga Tsutomu Katsuki Masaru Yamaguchi 《Tetrahedron letters》1981,22(8):773-774
Aromatic carotenoids, tedanin, agelaxanthin A, and tethyatene were synthesized from 0- acetyl-6-citraurin derived from natural zeaxanthin, and tethyatene was further transformed into renieratene as the first example of aromatization of an alicyclic ring in carotenoids. 相似文献
18.
Nada Kheira Sebbar Mohamed El Mehdi Mekhzoum El Mokhtar Essassi Abdelfettah Zerzouf Ahmed Talbaoui Youssef Bakri Mohamed Saadi Lahcen El Ammari 《Research on Chemical Intermediates》2016,42(9):6845-6862
In order to develop relatively small molecules as pharmacologically active molecules, novel 1,4-benzothiazine derivatives with triazole and oxazolidinone were synthesized. In this study, a series of 1,2,3-triazolylmethyl-1,4-benzothiazine derivatives were developed by exploiting a click chemistry reaction using a CuI-catalyzed Huisgen [3 + 2] cycloaddition. Starting from 2-(substituted)-3,4-dihydro-2H-1,4-benzothiazi-3-one, a number of 1,4-benzothiazine derivatives were also synthesized using different alkylating agents to give a 4-(substituted)-2-(substituted)-3,4-dihydro-2H-1,4-benzothiazi-3-one in good yields. The crystal and molecular structure of compound oxazolidin-2-one in basic benzothiazine was established by single-crystal X-ray diffraction. The newly synthesized products were subjected to in vitro biological evaluation. The result indicated that the compounds show convincing antibacterial activities against different microorganisms. All structures of the synthesized compounds were elucidated on the basis of spectral analyses and chemical reactions. 相似文献
19.
A variety of α-chloromethyl, α,α-dichloromethyl, and α,α,α-trichloromethyl ketones were synthesized from aldehyde utilizing cathodic reduction as key reactions. 相似文献
20.
Wenlong Yang Jorge H. S. K. Monteiro Ana deBettencourt‐Dias Vincent J. Catalano Wesley A. Chalifoux 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2016,128(35):10583-10586
The design of a relatively simple and efficient method to extend the π‐conjugation of readily available aromatics in one‐dimension is of significant value. In this paper, pyrenes, peropyrenes, and teropyrenes were synthesized through a double or quadruple benzannulation reaction of alkynes promoted by Brønsted acid. This novel method does not involve cyclodehydrogenation (oxidative aryl–aryl coupling) to arrive at the newly incorporated large arene moieties. All of the target compounds were synthesized in moderate to good yields and were fully characterized with the structures unambiguously confirmed by X‐ray crystallography. As expected, photophysical characterization clearly shows increasing red‐shifts as a function of extended conjugation within the fused ring systems. 相似文献