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81.
In this study, 1,3-disulfonic acid imidazolium hydrogen sulfate (DSIMHS) is used as an efficient and reusable ionic liquid for the green, mild, and efficient synthesis of xanthenes under solvent-free conditions. Simple and easy work-up, low cost, green process, short reaction times and excellent yields of the products are the advantages of this procedure. Further, the catalyst can be recycled and reused at least for four times without a noticeably decrease in its catalytic activity. 相似文献
82.
83.
Irum Shahzadi Ameer F. Zahoor Azhar Rasul Nasir Rasool Zohaib Raza Shahla Faisal Bushra Parveen Shagufta Kamal Muhammad Zia-ur-Rehman Faisal M. Zahid 《Journal of heterocyclic chemistry》2020,57(7):2782-2794
Theophylline-7-acetic acid (acefylline) ( 3 ) and its derivatives are pharmacologically active compounds and generally recognized as bronchodilators for the treatment of respiratory diseases like acute asthma for over 70 years. In this article, synthesis of 2-((5-((1,3-dimethyl-2,6-dioxo-2,3-dihydro-1H-purin-7(6H)-yl)methyl)-1,3,4-oxadiazol-2-yl)thio)-N-arylacetamides ( 10a-j ) has been reported. All the synthesized derivatives ( 10a-j) were structurally verified by FT-IR, 1H NMR, 13C NMR and evaluated for their anti-cancer (using MTT assay), hemolytic and thrombolytic potential. N-(4-Chlorophenyl)-2-(5-((1,3-dimethyl-2,6-dioxo-2,3-dihydro-1H-purin-7(6H)-yl)methyl)-1,3,4-oxadiazol-2-ylthio)acetamide ( 10g ) was found to be the most active against human liver cancer cell lines (Huh7) having cell viability 53.58 ± 1.28 using 100 μg/mL concentration of compound which was further in-silico modelled to describe the possible mechanistic insights for its anti-proliferative activity. The results of hemolytic and thrombolytic activities indicated that these derivatives were less toxic and hold considerable potential as a drug candidate. 2-(5-((1,3-Dimethyl-2,6-dioxo-2,3-dihydro-1H-purin-7(6H)-yl)methyl)-1,3,4-oxadiazol-2-ylthio)-N-(2-fluorophenyl)acetamide ( 10c ) of the series was found to be least toxic with 0.1% hemolysis relative to ABTS (95.5%) as positive control. 2-(5-((1,3-Dimethyl-2,6-dioxo-2,3-dihydro-1H-purin-7(6H)-yl)methyl)-1,3,4-oxadiazol-2-ylthio)-N-(tetrahydro-2H-pyran-4-yl)acetamide ( 10j ) exhibited potent clot lysis activity (90%) as compared to negative control DMSO (0.57%). 相似文献
84.
Nadhiratul-Farihin Semail Aemi Syazwani Abdul Keyon Bahruddin Saad Siti Salmah Noordin Nik Nur Syazni Nik Mohamed Kamal Nur Nadhirah Mohamad Zain 《液相色谱法及相关技术杂志》2020,43(15-16):562-579
Abstract5-fluorouracil (5-FU) refers to a fluorinated pyrimidine analogue that has been widely used as an anticancer agent for colon, head, and neck cancers. Detection of 5-FU and its metabolites; 5-fluorouridine and 5-fluoro-2-deoxyuridine in biological samples allows optimization of pharmacotherapy and encourages fundamental investigations of this medication. The development of accurate and reliable sample preparation, as well as analytical methods, is critical to isolate targeted analytes from complex matrices, apart from increasing detection sensitivity of analytes. With that, this paper presents a review of prior studies pertaining to chromatographic and electrophoretic methods that focused on the analysis of 5-FU and its metabolites in biological matrices such as plasma and urine. This paper concentrates on HPLC, GC and CE systems, which are the most commonly used strategies for analytical separation of 5-FU and its metabolites from samples. Detection of these antineoplastic agents at trace level demands highly sensitive and selective analytical methodologies. Application of these analytical techniques to biological matrices is reviewed with a focus on method development strategies, including types of mobile phases and background electrolytes employed in LC and CE systems. 相似文献
85.
Mandeep Kumar Arora Anish Ratra Syed Mohammed Basheeruddin Asdaq Ali A. Alshamrani Abdulkhaliq J. Alsalman Mehnaz Kamal Ritu Tomar Jagannath Sahoo Jangra Ashok Mohd Imran 《Molecules (Basel, Switzerland)》2022,27(6)
Plumbagin, a hydroxy-1,4-naphthoquinone, confers neuroprotection via antioxidant and anti-inflammatory properties. The present study aimed to assess the effect of plumbagin on behavioral and memory deficits induced by intrahippocampal administration of Quinolinic acid (QA) in male Wistar rats and reveal the associated mechanisms. QA (300 nM/4 μL in Normal saline) was administered i.c.v. in the hippocampus. QA administration caused depression-like behavior (forced swim test and tail suspension tests), anxiety-like behavior (open field test and elevated plus maze), and elevated anhedonia behavior (sucrose preference test). Furthermore, oxidative–nitrosative stress (increased nitrite content and lipid peroxidation with reduction of GSH), inflammation (increased IL-1β), cholinergic dysfunction, and mitochondrial complex (I, II, and IV) dysfunction were observed in the hippocampus region of QA-treated rats as compared to normal controls. Plumbagin (10 and 20 mg/kg; p.o.) treatment for 21 days significantly ameliorated behavioral and memory deficits in QA-administered rats. Moreover, plumbagin treatment restored the GSH level and reduced the MDA and nitrite level in the hippocampus. Furthermore, QA-induced cholinergic dysfunction and mitochondrial impairment were found to be ameliorated by plumbagin treatment. In conclusion, our results suggested that plumbagin offers a neuroprotective potential that could serve as a promising pharmacological approach to mitigate neurobehavioral changes associated with neurodegeneration. 相似文献
86.
Mahmoud Sunjuk Mousa Al-Noaimi Ghassan Abu Sheikha Ekkehard Lindner Bassam El-Eswed Kamal Sweidan 《Polyhedron》2009
Water-soluble functionalized bis(phosphine) ligands L (a–h) of the general formula CH2(CH2PR2)2, where for a: R = (CH2)6OH; b–g: R = (CH2)nP(O)(OEt)2, n = 2–6 and n = 8; h: R = (CH2)3NH2 ( Scheme 1), have been prepared photochemically by hydrophosphination of the corresponding 1-alkenes with H2P(CH2)3PH2. Water-soluble palladium complexes cis-[Pd(L)(OAc)2] (1–8) were obtained by the reaction of Pd(OAc)2 with the ligands a–h in a 1:1 mixture of dichloromethane:acetonitrile. The water-soluble phosphine ligands and their palladium complexes were characterized by IR, 1H and 31P NMR. A crystallographic study of complex 1 shows that the Pd(II) ion has a square planar coordination sphere in which the acetate ligands and the diphosphine ligand deviate by less than 0.12 Å from ideal planar. 相似文献
87.
Kamal YT Mohammed Musthaba S Singh M Parveen R Ahmad S Baboota S Ali I Siddiqui KM Arif Zaidi SM 《Biomedical chromatography : BMC》2012,26(10):1183-1190
An attempt has been made to develop and validate a simultaneous HPLC method for novel approach of drug release via oil‐in‐water (o/w) nanoemulsion formulation and Habb‐e‐Khardal Unani tablet containing piperine and guggul sterones E and Z as main ingredients. Nanoemulsion was prepared by titration method using sefsol‐218 as an oily phase, cremophor‐EL as a surfactant, transcutol as a co‐surfactant and distilled water as an aqueous phase. The formulation was optimized on the basis of thermodynamic stability and dispersibilty test. The nanoformulation was evaluated for particle size, surface morphology, electrical conductivity and viscosity determination. The in vitro dissolution was carried out by dialysis bag method. Drugs were quantified using an HPLC method developed in‐house with a C18 column as stationary phase and acetonitrile and water as mobile phase at λmax of 240 nm. The optimized formulation showed higher drug release, lower droplet size and less viscosity as compared with the conventional Habb‐e‐Khardal Unani tablet. The present study illustrated the potential of nanoemulsion dosage form in improving biopharmaceutic performance of piperine and guggul sterone. The HPLC method was also found to be quite sufficient for the routine quality control of formulations containing piperine and guggul sterone E and Z as ingredients and also for in vitro drug release studies. Copyright © 2011 John Wiley & Sons, Ltd. 相似文献
88.
Mohd Jailani Mohd Nor Mohammad Hosseini Fouladi Ahmad Kamal Ariffin 《Applied Acoustics》2008,69(4):343-353
Sound quality is among the main factors that influence customers’ preference for choosing good automobile products. It all started more than 10 years ago and grows up so fast due to high competition in the automotive industries. A-weighted noise levels and sound power are usually utilised to measure the noise but they are not adequate to characterise the impact sound inside a car. The most popular approach to determine sound quality of a product is to define an annoyance or specific index, which involves both subjective and objective evaluations. Subjective and objective tests should be studied concurrently in order to determine the sound quality inside a passenger car. This approach is used in this paper to evaluate vehicle comfort index according to most frequently used sound quality metrics, namely; Zwicker loudness, sharpness, roughness and fluctuation strength. As a result researchers of different fields of automotive acoustics investigations can use this index according to the type of road (international road roughness) without any need to perform time-consuming jury tests. The metrics are correlated with jury test results that show which of them and how much has affected the acoustical comfort of the vehicle. The relation between road roughness and vehicle acoustical comfort index is another point of interest in this research. 相似文献
89.
In this work, we investigate the emergence of rare and intense events during the Raman fiber amplification of a continuous wave. We highlight how dispersive properties and pump depletion can strongly influence the statistical properties of the amplified signal and its optical spectrum. Under certain conditions, the probability density functions of the amplified signal are calculated analytically and compared with the results of the numerical simulations. The conclusions are qualitatively validated by experiments carried out at telecommunication wavelengths. 相似文献
90.
Ashraf A. Aly Alaa A. Hassan Alan B. Brown Kamal M. El‐Shaieb Tarek M. I. Bedair 《Journal of heterocyclic chemistry》2011,48(4):787-791
New imidazoles were easily prepared from 2,3‐diamino‐1,4‐naphthoquinone and stoichiometric quantities of the appropriate aldehydes in dimethyl sulfoxide as a solvent. The reaction proceeded for few hours. The procedure can be generalized to different classes of aldehydes. 2‐Methyl‐1H‐naphtho[2,3‐d]imidazole‐4,9‐dione was also obtained in good yield during refluxing of 2,3‐diaminonaphthoquinone in acetic acid. The structure of the newly synthesized imidazoles was extensively investigated using NMR experiments. J. Heterocyclic Chem., (2011). 相似文献