Current organic synthesis最新文献

{"title":"Synthesis, Characterization and Preliminary Screening of New N-Substi-tuted -8-Methyl-4-Hydroxy-2-Quinolone -3-Carboxamides as Potential An-ticancer Agents","authors":"Dania Altaher, Hiba Zalloum, Kamal Sweidan, Dima A. Sabbah, Husam AlSalamat, Mahmoud Sunjuk, Reem Isleem","doi":"10.2174/0115701794291133240327044308","DOIUrl":"https://doi.org/10.2174/0115701794291133240327044308","url":null,"abstract":"Introduction: A new series of 4-hydroxy-8-methyl-2-oxo-1,2-dihydroquinoline-3-carboxamide derivatives has been synthesized in good yields, followed by complete characteri-zation using 1D-NMR, 2D-NMR, and IR techniques. Methods:: The final products contain amide, hydroxyl, and aromatic functional groups that usu-ally show significant bioactivity. The target products have been examined towards three cancer cell lines, namely colorectal cancer cell line (HCT116), breast cancer cell line (MCF-7), and leukemia cell line (K562) in addition to the fibroblast cells, that were used as a model for normal human tissue. Results:: The anticancer results signified that compound 6 showed the most activity in the series accomplished with IC50 values of 14.6, 5.3 and 12.8 μM, Conclusion:: Other compounds exhibited considerable activity, such as compounds 9 (IC50 3.5 and 19.0 μM), 10 (IC50 12.6 μM), and 11 (IC50 10.3 μM) against the three cancer cell lines HCT116, MCF-7 and K562, respectively.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"94 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-04-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140629863","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Stimuli-responsive Graphene-Polysaccharide Nanocomposites for Drug Delivery and Tissue Engineering","authors":"Arman Seifallahi Teymourlouei, Seyed Morteza Naghib, M. R. Mozafari","doi":"10.2174/0115701794298435240324175513","DOIUrl":"https://doi.org/10.2174/0115701794298435240324175513","url":null,"abstract":":: Natural polysaccharide-based nanoparticles are known for their non-toxic nature and diverse medical applications. Graphene oxide (GO) nanoparticles show potential in cancer treat-ment due to their ability to target medication delivery and influence ROS generation. These nanocomposites are versatile in gene transport, therapy, and photodynamic therapy, especially when surface-modified. Proper dispersion and functionalization of GO in polymer matrices are crucial, with examples like hyaluronic acid-functionalized GO offering versatile platforms for cancer drug administration. The potential of graphene oxide extends to cancer phototherapy, electronic nanowires, hydrogels, antibacterial nanocomposites, and environmental applications. When activated by polysaccharides, graphene-based nanocomposites exhibit anti-inflammatory and anticancer properties, making them valuable across various industries, including water treat-ment.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"203 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140570462","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"BODIPYs as Fluorogenic Probes for Live-Cell Imaging of Lipid Droplets: Photophysical and Computational Studies","authors":"Luana A. Machado, Cynthia L. M. Pereira, Ana Clara G. de Souza, Elivelton A. Ferreira, Flávia F. C. Marques, Ednilsom Orestes, Maria H. Araujo, Karen L. R. Paiva, Marina S. Mesquita, Sônia N. Báo, Leandro F. Pedrosa, Muhammad Jawad Nasim, Claus Jacob, Eufrânio N. da SilvaJúnior","doi":"10.2174/0115701794294862240322040633","DOIUrl":"https://doi.org/10.2174/0115701794294862240322040633","url":null,"abstract":"Introduction: Lipid droplets (LDs) serve as primary storage sites for neutral lipids within cells and are crucial for lipid metabolism. Disorders affecting LDs can contribute to the pathogenesis of common metabolic diseases such as obesity and can-cer, highlighting the importance of comprehending LD biology in health and disease contexts. background: Several synthetic methods for the preparation of BODIPYs are reported in the literature, yet the exploration of the different applications of this exciting class of fluorescent compounds is less studied and, therefore, a wide avenue of possibilities remains to be discovered. Methods: Fluorescence assays are commonly used for the detection and quantification of lipids in biological samples or lipid-rich environments. In this study, BODIPYs were synthesized and analyzed for structural confirmation. objective: synthesis of BODIPYs and evaluation of their affinity for intracellular lipid droplets Results: These compounds were subsequently evaluated for photophysical, electro-chemical (cyclic voltammetry) and theoretical analysis, followed by live-cell imaging studies to confirm their affinity for intracellular lipid droplets. method: In this study, BODIPYs were synthesized and analyzed for structural confirmation. These compounds were subsequently evaluated for photophysical, electrochemical (cyclic voltammetry) and theoretical analysis followed by live-cell imaging studies to confirm their affinity for intracellular lipid droplets. Conclusion: BODIPYs have been identified as fluorogenic probes for live-cell imag-ing studies and found to serve as efficient and selective fluorescent compounds for intracellular lipid droplets. result: BODIPYs have been identified as fluorogenic probes for live-cell imaging studies and found to serve as efficient and selective fluorescent compounds for intracellular lipid droplets.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"60 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140570464","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Investigation of the Effect of Power and Duration of Ultrasonic Irradiation on the Synthesis of Thiazoles","authors":"Eghlima Ehsani, Afshin Sarvary, Setareh Habibzadeh","doi":"10.2174/0115701794287558240220115823","DOIUrl":"https://doi.org/10.2174/0115701794287558240220115823","url":null,"abstract":"Introduction: The effect of power and duration of ultrasonic irradiation on the syn-thesis of thiazoles via the Hantzsch reaction was investigated. Methods: The reaction of phenacyl bromides with thioamides under ultrasonic irradiation af-forded the target thiazoles in good yields. Results: The results showed that high power and long irradiation time cause the decomposition of the reaction materials, and for this reaction, the irradiation power of 720 watts and a total duration of 4 minutes, wherein a pulsing function was performed in 50% of each second, were considered the most suitable irradiation properties for the synthesis of thiazoles through the Hantzsch reaction. Conclusion: The use of mild conditions, short time frame, high yields, simple separation of the reaction product, and no use of the base for neutralization are the advantages of the present method.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"109 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-04-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140570378","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Novel Pyridyl Macrocyclic Triarylmethanes: Synthesis by Ring-closing Metathesis and Chemical Analysis","authors":"Ameni Hadj Mohamed, Corinne Coutant, Moncef Msaddek, Maité Sylla-Iyarreta Veitía","doi":"10.2174/0115701794249707230930113307","DOIUrl":"https://doi.org/10.2174/0115701794249707230930113307","url":null,"abstract":"Background:: Nowadays, macrocyclic compounds constitute a privileged source for the development of compounds with interesting biological properties. Ring-closing olefin me-tathesis has received great attention for the synthesis of small, medium, and larger ring systems. Methods:: In the present work, we described the synthesis of eight original pyridyl macrocyclic triarylmethanes using an efficient 3-step synthetic strategy. The bisalkylated 4,4'-(pyridin-X-ylmethylene) diphenols (X=2-4) were prepared by ring-closing metathesis as macrocyclization key step, using Grubbs second generation catalyst. Results:: The pyridyl macrocyclic triarylmethanes were obtained with moderate to good yields. The introduction of a pyridine N-oxide moiety before the macrocyclization proved to be interest-ing to afford a higher yield of the corresponding metathesis product. FT-IR, 1 H NMR, 13C NMR, and X-ray diffraction analysis have been used for the characterization of the synthesized compounds. Conclusion:: The synthetic strategy used here proposes an efficient alternative to prepare macro-cyclic triarylmethanes of different sizes.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"57 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140570458","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Heteroaromatization of Coumarin Part II: Synthesis, Reactions, Antimicrobial Activities of Novel Pyrido[2,3-d]pyrimidine Derivatives","authors":"Rita M.A. Borik, Ashraf H. F. Abd El-Wahab, Hany M. M. Hamed, Khatib S. Ismail","doi":"10.2174/0115701794290718240322054346","DOIUrl":"https://doi.org/10.2174/0115701794290718240322054346","url":null,"abstract":"Background: Condensation of 3-acetyl-2H-chromen-2-one (1) with 2‐(4-methoxybenzylidene) malononitrile (2) in ammonium acetate/acetic acid or absolute ethanol/piperidine affords pyridine (3) and chromen-2-one (4) derivatives, respectively. background: Synthesis of a novel series of chromen-3-yl-pyridine derivatives were elucidated using spectroscopic techniques and elemental analysis. antimicrobial activities of compounds were then evaluated in vitro. Compound (E)-3-(3-(4-methoxyphenyl)acryloyl)-2H-chromen-2-one (4), was more effective against all five microorganisms and nicotinonitrile derivative 3 and 1,8-naphthyridin-2-yl)-2H-chromen-2-one derivative 14, while compounds 9, 10a-c, 11, 12 and 13 were moderate activity for antimicrobial activities. Methods: In this study, the reaction of 3 with an electrophilic reagent, namely, formic acid, acetic anhydride and formamide afforded the pyridopyrimidinone and pyridine derivatives (6- 9). Also, treatment of 3 with different aromatic aldehydes, carbon disulfide, NaN3/NH4Cl, 2- (4-methoxybenzylidene)malononitrile and acetophenone afforded pyridopyrimidinone, carbamodithioic acid, tetrazol-5-yl-chromen-2-one, 2H-chromen-2-one, and pyridine derivatives (10-14), respectively. Results: This study synthesized coumarins with antimicrobial activity and verified the structure and purity of the synthesized compounds using spectral data. Conclusion: The new compounds were evaluated in vitro for their antimicrobial activity against gram-positive bacteria (Staphylococcus aureus, Methicillin-resistant Staphylococcus aureus) and gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), in addition to fungus (Candida albicans). The investigated substances 3 and 14 presented good activity against MRSA, E. coli, P. aeruginosa and C. albicans, while compounds 9, 10a-c, 11, 12 and 13 exhibited good to moderate activity.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"117 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140570461","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Emerging Role of Polyethylene Glycol-Water (PEG-H2O) as the Benign Mixed Solvent System in Organic Synthesis","authors":"Chitteti Divyavani, Pannala Padmaja, Pedavenkatagari Narayana Reddy","doi":"10.2174/0115701794284081240206043435","DOIUrl":"https://doi.org/10.2174/0115701794284081240206043435","url":null,"abstract":": Polyethylene glycol (PEG) has become a popular solvent and green catalyst for a variety of chemical reactions. It is a stable and biodegradable polymeric catalyst used in organic synthesis because it may be recycled numerous times without significantly losing its catalytic activity. Recently, the use of PEG-H2O mixed solvent systems in organic synthesis has gained popularity. This article presents an overview of PEG-H2O solvent system-mediated organic reactions, with a main focus on the importance of the solvent system. The study also focuses on recent developments in the PEG-H2O solvent system-mediated synthesis of a number of heterocy-clic compounds. Important characteristics of these PEG-H2O solvent systems include high atom economies, gentle reaction conditions, faster reaction rates, readily isolated side products and high yields. Results from various reactions showed that the choice of proper ratio of PEG: H2O solvent system plays a key role in product yields.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"57-58 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-03-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140150169","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Study on the Catecholase Activity in the Presence of a Mn(III)-based Catalyst and Base","authors":"Rashmi Rekha Tripathy, Samaresh Jana, Sohini Sarkar","doi":"10.2174/0115701794285802240219064947","DOIUrl":"https://doi.org/10.2174/0115701794285802240219064947","url":null,"abstract":"Background:: This work describes the oxidation of a catechol moiety to the corresponding quinone by using Mn(III)-based catalysts in the presence of an organic base. Two newly reported Mn(III)-Schiff base complexes were utilized for the oxidation of three different substrates, namely, 3,5-di tert-butyl catechol, 1,4-dihydroxy benzene and pyrocatechol, aerobically. Objective:: We intended to understand the role of a base for the above-mentioned oxidation process. Also, we were interested to monitor the progress of reaction using 1H-NMR spectroscopy and to get more insight into the mechanistic path of the reaction. Methods:: The oxidation processes were studied in open air in acetonitrile or methanol solvent. The reaction mixture containing concerned substrate, catalyst, and base were stirred in open air and 1H-NMR spectrum was recorded using the crude reaction mixture in different time intervals. Results:: Interestingly, introduction of a base in the reaction mixture, enhanced the rate to a great extent for the first two substrates. This observation may provide an idea toward the rate determining step of the process. Notably, the third substrate, pyrocatechol, could not be oxidized by any of the two cata-lysts even with a base which might emphasize monodentate binding mode of the substrate. Each of the oxidation was monitored with the help of time dependent 1H-NMR spectroscopy. Conclusion:: A mechanistic pathway has been proposed. The spectra obtained in different cases help to compare the efficiency of the catalysts with or without base. In the absence of the catalysts, triethyl-amine alone cannot complete the conversion in the stipulated time, which may establish the effective-ness of the catalysts via the base-assisted mechanism.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"98 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-03-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140150064","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Alternative Method for the Selective Synthesis of Ortho-nitro Anilines Using Bismuth Nitrate Pentahydrate","authors":"Brenda V. Loera-García, Socorro Leyva-Ramos, Jaime Cardoso-Ortiz, Saúl Noriega, Antonio Romo-Mancillas, Kim M. Baines, Sarah L. McOnei","doi":"10.2174/0115701794273947231206111750","DOIUrl":"https://doi.org/10.2174/0115701794273947231206111750","url":null,"abstract":"Background: Nitroaromatic compounds are important scaffolds used for the syn-thesis of a variety of compounds, such as explosives, herbicides, dyes, perfumes and phar-maceuticals. Bismuth nitrate pentahydrate is a widely used reagent in organic synthesis; how-ever, its utility as a nitrating agent for anilines is underexplored. Objective: The aim of this work is to propose and find the proper reaction conditions of an alternative nitrating agent constituted by a mixture of bismuth nitrate / acetic anhydride in DCM with a series of substituted anilines under mild reflux. Methods: Several anilines having both activating and deactivating substituents in the ortho, meta and para positions were the substrate for the nitration reaction. Experimental conditions were performed in “one-pot” conditions before product purification. Results: Bi(NO3)3•5H2O demonstrated to be effective and somehow regioselective when it came to the nitration of anilines in the ortho position. Although other products were also identified under these conditions, in most cases, the ortho derivative was the major or even the only product obtained with moderate to high yields in the range of 50% – 96%. Conclusion: Bi(NO3)3•5H2O is an efficient and safe nitrating agent since the use of concen-trated and corrosive acids like sulfuric and nitric is avoided; furthermore, bismuth nitrate is low-priced and no special care nor equipment is required.","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":"1 1","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-02-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139945442","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Research Progress on the Application of Nanocellulose in Glucose Sensing.","authors":"Jianzhong Yuan, Caichao Wan, Song Wei, Huayun Chai, Tao Tao","doi":"10.2174/0115701794273511231212072414","DOIUrl":"https://doi.org/10.2174/0115701794273511231212072414","url":null,"abstract":"<p><strong>Background: </strong>Nanocellulose is not only a biocompatible and environmentally friendly material but also has excellent mechanical properties, biodegradability, and a large number of hydroxyl groups that have a strong affinity for water. These characteristics have attracted significant attention from researchers in the field of glucose sensing.</p><p><strong>Objective: </strong>This review provides a brief overview of the current research status of traditional materials used in glucose sensors. The sensing performance, chemical stability, and environ-mental properties of nanocellulose-based glucose sensors are compared and summarized based on the three sensing methods: electrochemical sensing, colorimetric sensing, and fluo-rescence sensing. The article focuses on recent strategies for glucose sensing using nanocel-lulose as a matrix. The development prospects of nanocellulose-based glucose sensors are also discussed.</p><p><strong>Conclusion: </strong>Nanocellulose has outstanding structural characteristics that contribute signifi-cantly to the sensing performance of glucose sensors in different detection modes. However, the preparation process for high-quality nanocellulose is complicated and has a low yield. Furthermore, the sensitivity and selectivity of nanocellulose-based glucose sensors require further improvement.</p>","PeriodicalId":11101,"journal":{"name":"Current organic synthesis","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2024-02-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139740637","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}