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101.
Chalcone-derived pyrimidine is a well-known heterocyclic compound that is commonly present in ribonucleic acid (RNA) and deoxyribonucleic acid (DNA) bio-isosteres. Pyrimidine derivatives are effective in both the electronic industry and drug industries. This review highlights the synthesis of pyrimidines, namely mono-pyrimidine, bis-pyrimidine, fused pyrimidine, symmetric, and asymmetric pyrimidine via one-pot and two-pot methods. The one-pot method is the direct reaction of amino derivatives with aldehydes and acetophenones, whereas the two-pot method is frequently reported for the synthesis of chalcone before the cyclization to a pyrimidine. This review is important in organic synthesis, particularly in the heterocyclic field, regarding pyrimidines and their significance in therapeutic and electronic industries. 相似文献
102.
Azizah M. Malebari Rakia Abd Alhameed Zainab Almarhoon Muhammad Farooq Mohammad A. M. Wadaan Anamika Sharma Beatriz G. de la Torre Fernando Albericio Ayman El-Faham 《Molecules (Basel, Switzerland)》2021,26(4)
Several derivatives containing morpholine/piperidine, anilines, and dipeptides as pending moieties were prepared using s-triazine as a scaffold. These compounds were evaluated for their anticancer activity against two human breast cancer cell lines (MCF-7 and MDA-MB-231), a colon cancer cell line (HCT-116), and a non-tumorigenic cell line (HEK 293). Tamoxifen was used as a reference. Animal toxicity tests were carried out in zebrafish embryos. Most of these compounds showed a higher activity against breast cancer than colon cancer. Compound 3a—which contains morpholine, aniline, and glycylglycinate methyl ester—showed a high level of cytotoxicity against MCF-7 cells with IC50 values of less than 1 µM. This compound showed a much lower level of toxicity against the non-tumorigenic HEK-293 cell line, and in the in vivo studies using zebrafish embryos. Furthermore, it induced cell cycle arrest at the G2/M phase, and apoptosis in MCF-7 cells. On the basis of our results, 3a emerges as a potential candidate for further development as a therapeutic drug to treat hormone receptor-positive breast cancer. 相似文献
103.
Prof. Dr. Antonino Gulino Prof. Dr. Georgia Papanikolaou Prof. Dr. Paola Lanzafame Prof. Dr. Abdellatif Aaliti Prof. Dr. Patrizia Primerano Prof. Dr. Luca Spitaleri Prof. Dr. Claudia Triolo Zainab Dahrouch Amani Khaskhoussi Prof. Dr. Sandra Lo Schiavo 《ChemistryOpen》2021,10(10):1033-1040
We report on the facile synthesis of SiO2@nitrized-TiO2 nanocomposite (NST) by calcination of TiO2 xerogel with OctaAmmonium POSS® (N-POSS; POSS=polyhedral oligomeric silsesquioxanes). The as-obtained nanoporous mixed oxide is constituted by uniformly distributed SiO2 and nitrized-TiO2, where the silica component is present in an amorphous state and TiO2 in an anatase/rutile mixed phase (92.1 % vs. 7.9 %, respectively) with very small anatase crystallites (3.7 nm). The TiO2 lattice is nitrized both at interstitial and substitutional positions. NST features a negatively charged surface with a remarkable surface area (406 m2 g−1), endowed with special adsorption capabilities towards cationic dyes. Its photocatalytic behavior was tested by following the degradation of standard aqueous methylene blue and methyl orange solutions under UV and visible light irradiation, according to ISO 10678:2010. For comparison, analogous investigations were carried out on a silica-free N−TiO2, obtained by using NH4Cl as nitrogen source. 相似文献
104.
Dr. Patrick M. J. Szell Zainab Rehman Ben P. Tatman Dr. Leslie P. Hughes Dr. Helen Blade Prof. Steven P. Brown 《Chemphyschem》2023,24(3):e202200558
Crystallographic disorder, whether static or dynamic, can be detrimental to the physical and chemical stability, ease of crystallization and dissolution rate of an active pharmaceutical ingredient. Disorder can result in a loss of manufacturing control leading to batch-to-batch variability and can lengthen the process of structural characterization. The range of NMR active nuclei makes solid-state NMR a unique technique for gaining nucleus-specific information about crystallographic disorder. Here, we explore the use of high-field 35Cl solid-state NMR at 23.5 T to characterize both static and dynamic crystallographic disorder: specifically, dynamic disorder occurring in duloxetine hydrochloride ( 1 ), static disorder in promethazine hydrochloride ( 2 ), and trifluoperazine dihydrochloride ( 3 ). In all structures, the presence of crystallographic disorder was confirmed by 13C cross-polarization magic-angle spinning (CPMAS) NMR and supported by GIPAW-DFT calculations, and in the case of 3 , 1H solid-state NMR provided additional confirmation. Applying 35Cl solid-state NMR to these compounds, we show that higher magnetic fields are beneficial for resolving the crystallographic disorder in 1 and 3 , while broad spectral features were observed in 2 even at higher fields. Combining the data obtained from 1H, 13C, and 35Cl NMR, we show that 3 exhibits a unique case of disorder involving the +N−H hydrogen positions of the piperazinium ring, driving the chloride anions to occupy three distinct sites. 相似文献
105.
Saira Khatoon Aggeliki Vgenopoulou Muhammad Moazzam Naseer Bahareh Shirinfar Benson M. Kariuki Necmi Dege Nisar Ahmed 《Journal of heterocyclic chemistry》2019,56(4):1388-1392
Several indoline derivatives with specific geometries are biologically active and have inhibitor properties. Many indolines are a key part of natural products. Much attention has been focused on the development of synthetic routes for their easy access. Current synthesis depends largely on metal catalysis, iodine reagents, and Oxone. To date, no synthetic route has been established that is metal‐free, reagent‐free, and environmentally friendly and provides a base for green chemistry. Here, we report the first facile metal‐free and reagent‐free synthesis of indoline derivatives, which could potentially be influential in the design of new biologically active compounds. The synthesis proceeds through intramolecular amination between a urea nucleophile and unactivated alkene. The ring closure occurs in a few hours in the presence of pre‐dried silica gel and gives good yields of indolines products, but in the absence of silica gel, the ring closure occurred overnight with stirring in dry solvent. An electron withdrawing group at the substituted aryl moiety of ureas increases the hydrogen bond donor ability of substrates that mediate the internal proton transfer at the terminal alkene and results in facile amination to give the indoline product with an “in plane” orientation of the carbonyl group and aromatic part of indoline framework. Such orientation in indolines is important for potent biological activities. 相似文献
106.
A series of organotin(IV) thiocarboxylates have been synthesized with the general formula R2SnL2 and R3SnL (R = Ph2(I), Me3(II), n‐Bu3(III), Ph3(IV), Cy3(V), Me2(VI), n‐Bu2(VII), and L = piperidine‐1‐thiocarboxylic acid) in anhydrous toluene under the reflux conditions. The complexes were characterized by microanalysis, IR, 1H and 13C NMR, mass spectrometry, and XRD. NMR data revealed that thiocarboxylic acid acts as bidentate, and complexes exhibit the four‐coordinated geometry in solution state. In solid state, diorganotin complexes exhibit the hexa‐coordinated geometry whereas the triorganotin(IV) compounds show the five‐coordinated geometry. These complexes were also tested for their antimicrobial activity along with the ligand against different animals, plant pathogens, and Artemia salina. All complexes with few exceptions show high activity as compared to the ligand. © 2007 Wiley Periodicals, Inc. Heteroatom Chem 18:664–674, 2007; Published online in Wiley InterScience ( www.interscience.wiley.com ). DOI 10.1002/hc.20380 相似文献
107.
Rizwan Ahmad Niyaz Ahmad Mohd Amir Fatema Aljishi Marwah Hussain Alamer Heba Radhi Al-Shaban Zainab Alawi Alsadah Bayan Mohammed Alsultan Noor Ali Aldawood Shahanas Chathoth Sarah Ameen Almofty 《Biomedical chromatography : BMC》2020,34(3):e4772
Black pepper (Piper nigrum; BP), known as the ‘king of spices’, imported from various countries is widely available in Saudi Arabian markets, as its demand as a food as well as a medicine for minor ailments is increasing in the country. However, there is a lack of appropriate information regarding these samples in terms of quality variation and standardization. We thus aimed to evaluate the quality and standardize the BP sample with respect to its physicochemical characters, active principle variation [i.e. piperine (PPN)], toxicity, and biological activity. The main focus is to validate whether any difference exists in the quality and quantity of active principle in these samples. For this purpose, physicochemical (chemical tests and ash values) and instrumental analyses [accelerated solvent extraction (ASE), ultra-high-pressure liquid chromatography (UHPLC)-diode array detector, infrared (IR), nuclear magnetic resonance (NMR), and inductively coupled plasma-MS (ICP-MS)] and biological evaluation {in vitro antioxidant activity [2,2-diphenyl-1-picrylhydrazyl and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)] and cytotoxicity assay} were performed. An extract yield (g) with %recovery of 2.26 ± 4.24 (11.3) was obtained for the Vietnamese sample, using a fast and rapid method of extraction (ASE). These values were 1.22 ± 2.64 (6.1) and 0.75 ± 1.69 (3.75) for the Pakistani and Indian samples. Physicochemical tests revealed the presence of flavonoids and phenolic compounds in all samples; however, in the Vietnamese sample a low amount of total, acid-insoluble, and high water-soluble ash value was noted. IR and NMR was applied to further standardize the samples. Results of ICP-MS analysis showed a high amount of macronutrients and micronutrients in the samples tested while UHPLC analysis revealed a high amount of PPN (ng/mL) in the Pakistani sample (1,362,614.09); these values were 1,051,848.04 and 768,512.81 for the Vietnamese and Indian samples, respectively. In vitro antioxidant and cytotoxicity activities revealed higher potential for the Vietnamese sample. The samples were properly standardized and effectively differentiated in terms of quality and biological activities using a fast and reliable method, however it certainly does not mean that a particular geographical region is more better or productive in terms of herbal products. 相似文献
108.
Muhammad Ashraf Syed Shaheen Shah Dr. Ibrahim Khan Dr. Md. Abdul Aziz Prof. Nisar Ullah Dr. Mujeeb Khan Dr. Syed Farooq Adil Zainab Liaqat Dr. Muhammad Usman Prof. Wolfgang Tremel Dr. Muhammad Nawaz Tahir 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(23):6973-6984
Tungsten oxide/graphene hybrid materials are attractive semiconductors for energy-related applications. Herein, we report an asymmetric supercapacitor (ASC, HRG//m-WO3 ASC), fabricated from monoclinic tungsten oxide (m-WO3) nanoplates as a negative electrode and highly reduced graphene oxide (HRG) as a positive electrode material. The supercapacitor performance of the prepared electrodes was evaluated in an aqueous electrolyte (1 m H2SO4) using three- and two-electrode systems. The HRG//m-WO3 ASC exhibits a maximum specific capacitance of 389 F g−1 at a current density of 0.5 A g−1, with an associated high energy density of 93 Wh kg−1 at a power density of 500 W kg−1 in a wide 1.6 V operating potential window. In addition, the HRG//m-WO3 ASC displays long-term cycling stability, maintaining 92 % of the original specific capacitance after 5000 galvanostatic charge–discharge cycles. The m-WO3 nanoplates were prepared hydrothermally while HRG was synthesized by a modified Hummers method. 相似文献
109.
Islam Shumaila Bakhtiar Hazri Riaz Saira Naseem Shahzad 《Journal of Sol-Gel Science and Technology》2021,100(1):192-204
Journal of Sol-Gel Science and Technology - Sol–gel-based phenolphthalein immobilized AuNPs (phph-AuNPs) of different shapes such as spherical, dendrites, and flower are observed by varying... 相似文献
110.
Malik Fariha Butt Saira Mujahid Nouman 《Journal of Radioanalytical and Nuclear Chemistry》2022,331(2):683-690
Journal of Radioanalytical and Nuclear Chemistry - The stable isotopic contents of precipitation and deuterium excess (d-excess) data justified the hypothesis that two distinct vapor sources are... 相似文献