Current Chemistry Letters最新文献

Design, synthesis and characterization of some new pyrazol-pyrimidine derivatives and evaluation of their biological activities 一些新的吡唑-嘧啶衍生物的设计、合成、表征及其生物活性评价

Current Chemistry Letters Pub Date : 2023-01-01 DOI: 10.5267/j.ccl.2023.2.004

R. Rani, T. Venkatesh, N. Satyanarayan, B. N. Nippu

引用次数: 0

Quantification of Alectinib in spiked rabbit plasma using liquid chromatography- electro spray ionization-tandem mass spectrophotometry: An application to pharmacokinetic study 液相色谱-电喷雾电离-串联质谱法定量家兔血浆中阿勒替尼的药代动力学研究

Current Chemistry Letters Pub Date : 2023-01-01 DOI: 10.5267/j.ccl.2023.1.002

H. Kumar, S. Acharyya, P. Mondal, P. Patra, Satyabrata Sahu

{"title":"Quantification of Alectinib in spiked rabbit plasma using liquid chromatography- electro spray ionization-tandem mass spectrophotometry: An application to pharmacokinetic study","authors":"H. Kumar, S. Acharyya, P. Mondal, P. Patra, Satyabrata Sahu","doi":"10.5267/j.ccl.2023.1.002","DOIUrl":"https://doi.org/10.5267/j.ccl.2023.1.002","url":null,"abstract":"The current technique was developed to estimate the amount of alectinib present in spiked rabbit plasma using liquid chromatographic mass spectrometry. The liquid-liquid extraction method was used, and chromatographic separation was carried out on a C18 (4.6mm id x 50mm) analytical column with a mobile phase consisting of acetonitrile and water with 0.1% formic acid at a volume ratio of 75:25. Alectinib's product m/z +483.2 (parent) 396.1 (product) and the internal standard m/z +447.5 (parent) 380.3 (product) were both obtained using positive ion mode. The calibration curve was linear from 0.5 to 600 ng/ml. The percentage extraction recovery (98.15% → 98.86%), demonstrated excellent matrix and analyte selectivity (% interference = 0), and satisfactory stability study results in all types (% nominal 94.94% → 99.63%). The intra and interday accuracy with % nominal 97 → 98.8%, precision % CV ≤ 2% in all quality control levels. The rabbit model's pharmacokinetic parameters were examined, and alectinib's area under the curve (AUC 0—∞) was 4269 ± 8.13 hr.ng/ml. The half-life of elimination (t1/2) is 8.52 ± 6.66 hours. The currently established approach was used in rabbit blood samples for pharmacokinetic investigations of commercial formulations since it was thought to be a novel, verified bioanalytical method based on experimental results.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"170 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73424965","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Design, synthesis, molecular docking and biological evaluation of some pyridinone bearing scaffold benzofuran as antimicrobial and antioxidant activity 吡啶酮承载支架苯并呋喃的设计、合成、分子对接及生物学评价

Current Chemistry Letters Pub Date : 2023-01-01 DOI: 10.5267/j.ccl.2022.8.008

Bharathi Sharanappa Veerapur, L.N. Netravati, H.M. Naveenakumari, K. Basavaraja

引用次数: 0

Studies of kinetic models and adsorption isotherms: application on the interaction of insulin with synthetic hydroxyapatite 动力学模型和吸附等温线的研究:胰岛素与合成羟基磷灰石相互作用的应用

Current Chemistry Letters Pub Date : 2023-01-01 DOI: 10.5267/j.ccl.2022.11.001

A. E. Rhilassi, M. B. Ziatni

{"title":"Studies of kinetic models and adsorption isotherms: application on the interaction of insulin with synthetic hydroxyapatite","authors":"A. E. Rhilassi, M. B. Ziatni","doi":"10.5267/j.ccl.2022.11.001","DOIUrl":"https://doi.org/10.5267/j.ccl.2022.11.001","url":null,"abstract":"The non-stoichiometric, calcium-deficient hydroxyapatite was prepared through a low-temperature from aqueous solutions method and characterized using Physico-chemical methods. The potential of this hydroxyapatite to adsorb and release insulin from aqueous solutions was evaluated under physiological conditions. The effect of contact time and initial concentration were studied in batch experiments. The adsorption rate reached up to 81±5% in the first half-hour of contact, while the release rate of insulin incubation was about 41 ± 5% after 1 hour. The pseudo-first-order, pseudo-second-order, Elovich equation, Weber and Morris intraparticle diffusion model and Bangham’s pore diffusion model were applied to study the kinetics of the adsorption process. The pseudo-second-order kinetic model provided the best correlation R2(0.998) of the used experimental data compared to the other models. The adsorption of insulin onto hydroxyapatite was correlated well R2(0.998) with the Langmuir model as compared to Freundlich, Temkin and Dubinin–Kaganer–Radushkevich (D-K-R) models, with a maximum adsorption capacity of 24.46 mg/g. The isotherms parameters values of ΔG0, b_t and E show that the adsorption process is favorable, spontaneous, exothermic, and controlled by physisorption. The point of zero charge (pHZPC) of hydroxyapatite and the isoelectric point (pI) of insulin indicate that the interaction of insulin molecules with prepared apatite can be well described as an ions exchange reaction.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"12 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77226403","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

In silico molecular docking study and Protective effect of Piper attenuatum on aspirin induced gastric ulcer in rats 薄叶胡椒对阿司匹林致大鼠胃溃疡的保护作用及其分子对接研究

Current Chemistry Letters Pub Date : 2023-01-01 DOI: 10.5267/j.ccl.2023.5.004

G. Soni, Shikha Sharma, Neha Dangi

{"title":"In silico molecular docking study and Protective effect of Piper attenuatum on aspirin induced gastric ulcer in rats","authors":"G. Soni, Shikha Sharma, Neha Dangi","doi":"10.5267/j.ccl.2023.5.004","DOIUrl":"https://doi.org/10.5267/j.ccl.2023.5.004","url":null,"abstract":"Steroid and painkiller abuse induced peptic ulcer disease, which causes abdominal pain, fullness, heartburn, and nausea. Medicinal plants have treated ulcers for centuries. We used Piper attenuatum ethanolic plant extracts for aspirin to induce ulcers in Wistar rats to test the leaf ethanolic extract's antiulcer properties. The control group is normal saline, the standard group is ranitidine (20 mg/kg), and the extract-treated groups are 100 mg/kg and 200 mg/kg ethanolic plant extracts. Ulcer Score, gastric juice volume, free and total acidity, ulcer index, ulcer protection, and pH were measured. The ulcer score was determined via rat stomach biopsies. Plant ethanolic extracts are gastroprotective. Only pH increased compared to the control group. Piper attenuatum ethanolic extract is the most gastroprotective at 200 mg/kg. Extracts were phytochemically and analytically assessed. Phytochemical screening demonstrates that plant extracts contain alkaloids, amides, glucose, proteins, glycosides, steroids, flavonoids, etc. This research suggests that phytoconstituents may have anti-ulcer potential, although structural elucidation of bioactive chemicals is needed. Molecular docking showed better binding affinity versus the 3D structure of pig gastric H+/K+ ATPase isoforms phytoconstituents Cepharadione A, Cepharadione B, Guineensine, Norcepharadione B, and Piperlonguminine. With these significant results, it may be a drug in the future.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82397735","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Synthesis and evaluation of antimicrobial activity of some new 3-(pyrrol-4-yl)acrylamide derivatives 新型3-(吡咯-4-酰基)丙烯酰胺衍生物的合成及抗菌活性评价

Current Chemistry Letters Pub Date : 2023-01-01 DOI: 10.5267/j.ccl.2023.3.004

S. Kemskyi, M. Fedoriv, A. Palamar, A. Grozav, V. Chornous, R. Kutsyk, V. Dorokhov, M. Vovk

{"title":"Synthesis and evaluation of antimicrobial activity of some new 3-(pyrrol-4-yl)acrylamide derivatives","authors":"S. Kemskyi, M. Fedoriv, A. Palamar, A. Grozav, V. Chornous, R. Kutsyk, V. Dorokhov, M. Vovk","doi":"10.5267/j.ccl.2023.3.004","DOIUrl":"https://doi.org/10.5267/j.ccl.2023.3.004","url":null,"abstract":"A series of new derivatives of 3-(pyrrol-4-yl)acrylamides 3a-l with the pyrrole nucleus functionalized by chlorine atoms and ester group, have been synthesized by simple preparative methods from the available esters of 5-chloro-4-formylpyrrol-3-carboxylic acids 1a-e. At first, 3-(pyrrol-4-yl)acrylic acids 2a-e were synthesized by the Knoevenagel’s reaction between malonic acid and the esters 1a-e. Then the target compounds were obtained with a high yield in the reactions between chloroanhydrides of the synthesized acrylic acids and aromatic or aliphatic amines in the boiling benzene. The structure of all obtained compounds was confirmed by elemental analysis, IR, 1H-NMR, and 13C-NMR spectroscopy, and additionally checked by the mass-spectrometry. Then the antimicrobial activity of all amides was tested in vitro on some gram-positive and gram-negative bacteria and fungi. It has been found that the gram-negative bacteria are resistant against the synthesized chemicals, while the gram-positive bacteria are sensitive to the amides 3с, e, f, g, i. The highest activity against Staphylococcus aureus MR and Staphylococcus epidermidis MS was registered for the amide 3f, and the retardation area diameter for this amide was greater than that for the control drugs.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"67 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87510232","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Evaluation of methyl red removal potential of adsorbents made from Leucaena leucocephala leaf and bark materials 银合欢叶和树皮材料吸附剂去除甲基红的潜力评价

Current Chemistry Letters Pub Date : 2023-01-01 DOI: 10.5267/j.ccl.2022.8.001

Venkata Kishore Babu Chukka, Venkata Ramana Kokkiligadda, R. Brahmaji, H. Bollikolla

引用次数: 0

Green synthesis, characterization, and biological activities of Zn, Cu monometallic and bimetallic nanoparticles using Borassus flabellifer leaves extract 竹叶提取物制备锌、铜单金属和双金属纳米粒子的绿色合成、表征及生物活性研究

Current Chemistry Letters Pub Date : 2023-01-01 DOI: 10.5267/j.ccl.2023.4.002

S. Dubey, A. Shukla, R. Shukla

{"title":"Green synthesis, characterization, and biological activities of Zn, Cu monometallic and bimetallic nanoparticles using Borassus flabellifer leaves extract","authors":"S. Dubey, A. Shukla, R. Shukla","doi":"10.5267/j.ccl.2023.4.002","DOIUrl":"https://doi.org/10.5267/j.ccl.2023.4.002","url":null,"abstract":"In the present work, Zn, Cu monometallic and bimetallic nanoparticles were synthesized using leaves extract of Borassus flabellifer. Plant extract acts as both surfactant and reducing agent. The synthesized nanoparticles were characterised by UV-Vis, XRD, FESEM, EDX, and HRTEM techniques. UV-Vis spectroscopy is used to monitor the synthesis of nanoparticles. XRD technique was used to confirm the amorphous nature of nanoparticles. The FESEM images demonstrate that the shape of the nanoparticles such as Zn monometallic (pseudo-spherical), Cu monometallic (rod), Zn-Cu bimetallic are (pseudo-spherical and rod-shaped). HRTEM images show the approximate size of the Zn, Cu monometallic and Zn-Cu bimetallic nanoparticles is 3.0 nm, 3.52 nm and 2.2 nm respectively. EDX spectra confirm the presence of Zn, Cu and O in the sample. Synthesized Zn, Cu monometallic nanoparticles, and Zn-Cu bimetallic nanoparticles were used to evaluate their possible antimicrobial, antidiabetic and antioxidant properties. Bimetallic nanoparticles displayed higher antioxidant, antidiabetic, and antimicrobial properties in the comparison of monometallic nanoparticles. The results suggest that Zn-Cu bimetallic nanoparticles have greater potential than monometallic nanoparticles.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"40 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83637566","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Effect of thermal requirements on chemical content of sugar beet and it’s reflecting on yield in Upper Egypt 上埃及地区热需要量对甜菜化学成分的影响及其对产量的反映

Current Chemistry Letters Pub Date : 2023-01-01 DOI: 10.5267/j.ccl.2023.1.006

Omar M. Yassin, S. Ismail, M. Gameh, F. Khalil, Ezzat M. Ahmed

引用次数: 0

Crystal structure, DFT, molecular docking and dynamics simulation studies of 4,4-dimethoxychalcone 4,4-二甲氧基查尔酮的晶体结构、DFT、分子对接及动力学模拟研究

Current Chemistry Letters Pub Date : 2023-01-01 DOI: 10.5267/j.ccl.2023.2.006

M. V. Gowda, B. Vinay, N. Maitra, S. Kumaraswamy, N. Lokanath

{"title":"Crystal structure, DFT, molecular docking and dynamics simulation studies of 4,4-dimethoxychalcone","authors":"M. V. Gowda, B. Vinay, N. Maitra, S. Kumaraswamy, N. Lokanath","doi":"10.5267/j.ccl.2023.2.006","DOIUrl":"https://doi.org/10.5267/j.ccl.2023.2.006","url":null,"abstract":"In the current study, the compound 4,4-dimethoxychalcone (DMC) was structurally studied and analyzed by in silico approach against Mpro to investigate its inhibitory potential. The molecular structure of the compound was confirmed by the single crystal X-ray diffraction studies. The crystal structure packing is characterized by various hydrogen bonds, C-H…π and π…π stacking. Intermolecular interactions are quantified by Hirshfeld surface analysis and the electronic structure was optimized by DFT calculations; results are in agreement with the experimental studies. Further, DMC was virtually screened against SARS-CoV-2 main protease (PDB-ID: 6LU7) using molecular docking, and molecular dynamics (MD) simulations to identify its inhibitory potential. A significant binding affinity exists between DMC and Mpro with a -6.00 kcal/mol binding energy. A MD simulation of 30ns was carried out; the results predict DMC possessing strong binding affinity and hydrogen-bonding interactions within the active site during the simulation period. Therefore, based on the results of the current investigation, it can be inferred that a DMC molecule may be able to inhibit Mpro of COVID-19.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"43 1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75404975","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0