Russian Journal of General Chemistry最新文献

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Design and Synthesis of Novel Betulin Derivatives Containing Thiazole Moiety as Anticancer Agents 含噻唑基团新型抗癌白桦林衍生物的设计与合成
IF 0.9 4区 化学
Russian Journal of General Chemistry Pub Date : 2025-03-27 DOI: 10.1134/S1070363224613206
Y. B. Zhang, S. W. Pan, M. Zhang, X. S. Guo, J. F. Wang, M. Bu
{"title":"Design and Synthesis of Novel Betulin Derivatives Containing Thiazole Moiety as Anticancer Agents","authors":"Y. B. Zhang,&nbsp;S. W. Pan,&nbsp;M. Zhang,&nbsp;X. S. Guo,&nbsp;J. F. Wang,&nbsp;M. Bu","doi":"10.1134/S1070363224613206","DOIUrl":"10.1134/S1070363224613206","url":null,"abstract":"<p>A series of novel betulin-28-thiazole ester derivatives were designed, synthesized, and subsequently evaluated for their anticancer activity. Among these compounds, 3β-hydroxylup-20(29)-en-28-yl 3-(5-carboxy-4-methylthiazol-2-yl)-1-methylpyridin-1-ium iodide demonstrated the most potent anticancer activity against A549 cells, with an IC<sub>50</sub> value of 2.24 µM, being 11.23-fold more potent than betulin. Meanwhile, 3β-hydroxylup-20(29)-en-28-yl 3-(5-carboxy-4-methylthiazol-2-yl)-1-methylpyridin-1-ium iodide displayed exceptional water solubility, being 20.15-fold higher than that of betulin. In summary, these data identified 3β-hydroxylup-20(29)-en-28-yl-3-(5-carboxy-4-methylthiazol-2-yl)-1-methylpyridin-1-ium iodide as a promising lead compound that warrants further investigation of its anticancer properties.</p>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"95 3","pages":"679 - 689"},"PeriodicalIF":0.9,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143716794","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}
引用次数: 0
New 4-Thiazolidinone-Bearing Fluoroquinolone Derivatives: Synthesis, Antimicrobial Effectiveness, Structural Characterization, and In Silico Docking Analysis 新的含4-噻唑烷酮类氟喹诺酮衍生物:合成、抗菌有效性、结构表征和硅对接分析
IF 0.9 4区 化学
Russian Journal of General Chemistry Pub Date : 2025-03-27 DOI: 10.1134/S1070363224612754
V. S. P. K. Gudapati, S. R. Basireddy, D. V. P. K. Gudapati, M. Afzal, A. Ayub, S. K. Kolli
{"title":"New 4-Thiazolidinone-Bearing Fluoroquinolone Derivatives: Synthesis, Antimicrobial Effectiveness, Structural Characterization, and In Silico Docking Analysis","authors":"V. S. P. K. Gudapati,&nbsp;S. R. Basireddy,&nbsp;D. V. P. K. Gudapati,&nbsp;M. Afzal,&nbsp;A. Ayub,&nbsp;S. K. Kolli","doi":"10.1134/S1070363224612754","DOIUrl":"10.1134/S1070363224612754","url":null,"abstract":"<p>A series of ciprofloxacin-based thiazolidinone derivatives were developed and prepared by reacting active methylene compound with corresponding aldehydes. The novel compounds were analyzed using several spectroscopic techniques (FT-IR, <sup>1</sup>H, <sup>13</sup>C NMR and MS), and their antimicrobial properties were tested. Their minimum inhibitory concentration values were between 1.6 and 72.1 µg/mL, similar to MXF (1.9–3.5 µg/mL). From screening, the antibacterial results showed that <i>p</i>-chlorobenzylidene, <i>p</i>-dimethylaminobenzylidene, and <i>m</i>-methoxybenzylidene derivatives showed outstanding antibacterial activity against <i>E. coli</i> with zone of inhibition values of 27±0.1, 21±0.1, and 22±0.3 mm, respectively. The molecular docking predictions showed that the most active compounds have good binding affinities with <i>E. coli</i> DNA gyrase (7C7N). ADMET predictions were performed; the most thiazolidines possess the highest drug likeness score (1.23–1.61) as a promising pharmacokinetic safety profile.</p>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"95 3","pages":"630 - 643"},"PeriodicalIF":0.9,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143716882","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}
引用次数: 0
Synthesis of Novel Substituted 4-[1-(1-Phenyl-1H-[1,2,3]triazol-4-yl-methyl)-1H-benzimidazol-2-yl]piperidine-1-carboxylic Acids tert-Butyl Esters. Evaluation of Cytotoxic and Antimicrobial Activity 新型取代4-[1-(1-苯基- 1h -[1,2,3]三唑-4-基甲基)- 1h -苯并咪唑-2-基]哌啶-1-羧酸叔丁基酯的合成。细胞毒性和抗菌活性评价
IF 0.9 4区 化学
Russian Journal of General Chemistry Pub Date : 2025-03-27 DOI: 10.1134/S1070363224611293
P. Naresh, Y. Hemasri, P. Limbadri, Y. Jayaprakash Rao
{"title":"Synthesis of Novel Substituted 4-[1-(1-Phenyl-1H-[1,2,3]triazol-4-yl-methyl)-1H-benzimidazol-2-yl]piperidine-1-carboxylic Acids tert-Butyl Esters. Evaluation of Cytotoxic and Antimicrobial Activity","authors":"P. Naresh,&nbsp;Y. Hemasri,&nbsp;P. Limbadri,&nbsp;Y. Jayaprakash Rao","doi":"10.1134/S1070363224611293","DOIUrl":"10.1134/S1070363224611293","url":null,"abstract":"<p>A straightforward and effective method for the synthesis of new series of benzimidazole-triazole hybrids developed by adopting click Cu(I)-catalyzed 1,3-dipolar cycloaddition. Alkyne tethered benzimidazole carboxylates treated with various aromatic azides using sodium ascorbate and copper sulphate as catalytic medium. The resulting series of novel benzimidazole-linked 1,2,3-triazole analogues were characterized using NMR, IR, mass spectral data. All the compounds screened for cytotoxic and antimicrobial activity. Three compounds exhibited good cytotoxic as well as antimicrobial activity</p>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"95 3","pages":"538 - 547"},"PeriodicalIF":0.9,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143716667","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}
引用次数: 0
Cobalt(II) Complexes with Fluorinated β-Diketones and Their Derivatives for MOCVD Applications 钴(II)与氟化β-二酮配合物及其衍生物在MOCVD中的应用
IF 0.9 4区 化学
Russian Journal of General Chemistry Pub Date : 2025-03-27 DOI: 10.1134/S1070363224613292
S. I. Dorovskikh, A. S. Sukhikh, V. A. Yatygin, A. E. Turgambaeva, E. A. Maximovskiy, D. P. Pishchur, E. S. Vikulova
{"title":"Cobalt(II) Complexes with Fluorinated β-Diketones and Their Derivatives for MOCVD Applications","authors":"S. I. Dorovskikh,&nbsp;A. S. Sukhikh,&nbsp;V. A. Yatygin,&nbsp;A. E. Turgambaeva,&nbsp;E. A. Maximovskiy,&nbsp;D. P. Pishchur,&nbsp;E. S. Vikulova","doi":"10.1134/S1070363224613292","DOIUrl":"10.1134/S1070363224613292","url":null,"abstract":"<p>A series of new volatile cobalt(II) chelates with ligands containing an extended perfluoroalkyl group, [CH<sub>3</sub>C(X)CHC(O)R]<sup>–</sup>, R = C<sub>2</sub>F<sub>5</sub>, X = O (L<sup>1</sup>) or NH (NL<sup>1</sup>); R = C<sub>3</sub>F<sub>7</sub>, X = O (L<sup>2</sup>) or NH (NL<sup>2</sup>), were obtained via a salt metathesis reaction. Elemental analysis and IR spectroscopy were used to confirm the formation of heteroligand complexes [Со(H<sub>2</sub>O)<sub>2</sub>(L<sup>1</sup>)<sub>2</sub>] and [Со(H<sub>2</sub>O)<sub>2</sub>(L<sup>2</sup>)<sub>2</sub>]·<i>n</i>H<sub>2</sub>O (<i>n</i> = 1, 2) in the case of β-diketonates, while homoligand complexes [Со(NL<sup>1</sup>)<sub>2</sub>] and [Со(NL<sup>2</sup>)<sub>2</sub>] were obtained for β-iminoketonates. Single-crystal X-ray diffraction revealed the structures of [Со(CH<sub>3</sub>OH)<sub>2</sub>(L<sup>1</sup>)<sub>2</sub>] (Im, CCDC 2374366) and [Со(H<sub>2</sub>O)<sub>2</sub>(L<sup>2</sup>)<sub>2</sub>]·H<sub>2</sub>O (CCDC 2374367), and comparison with related compounds allowed for the identification of specific structural features of heteroligand cobalt(II) complexes. The thermal behavior of the synthesized complexes was investigated using thermogravimetry and differential scanning calorimetry. The feasibility of chemical vapor deposition of Cо<sub>3</sub>О<sub>4</sub> nanomaterials from [Со(NL<sup>1</sup>)<sub>2</sub>]. was demonstrated. The obtained samples were characterized by X-ray phase analysis, Raman spectroscopy, and scanning electron microscopy.</p>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"95 3","pages":"690 - 703"},"PeriodicalIF":0.9,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143716856","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}
引用次数: 0
Erratum to: Microwave-Assisted Facile Synthesis of 1,2-Benzisoxazoles, Isoxazoloquinolines, and Isothiazoloquinolines in [BMIM(SO2Cl)][OTs] Ionic Liquid as a Recyclable System [BMIM(SO2Cl)][OTs]离子液体中微波辅助快速合成1,2-苯并异恶唑、异恶唑喹啉和异噻唑喹啉
IF 0.9 4区 化学
Russian Journal of General Chemistry Pub Date : 2025-03-27 DOI: 10.1134/S1070363225030272
I. Jamadar, R. B. Manami, S. Kurahatti, A. Anchi, V. Jadhav, R. G. Kalkhambkar, M. Kurkuri, M. S. Refat, A. M. Alsuhaibani
{"title":"Erratum to: Microwave-Assisted Facile Synthesis of 1,2-Benzisoxazoles, Isoxazoloquinolines, and Isothiazoloquinolines in [BMIM(SO2Cl)][OTs] Ionic Liquid as a Recyclable System","authors":"I. Jamadar,&nbsp;R. B. Manami,&nbsp;S. Kurahatti,&nbsp;A. Anchi,&nbsp;V. Jadhav,&nbsp;R. G. Kalkhambkar,&nbsp;M. Kurkuri,&nbsp;M. S. Refat,&nbsp;A. M. Alsuhaibani","doi":"10.1134/S1070363225030272","DOIUrl":"10.1134/S1070363225030272","url":null,"abstract":"","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"95 3","pages":"781 - 781"},"PeriodicalIF":0.9,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143716702","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}
引用次数: 0
Synthesis and Properties of Phthalonitriles with 2-Phenylphenoxy Groups and Corresponding Metallophthalocyanines 2-苯基苯氧基酞腈及其金属酞菁的合成与性能研究
IF 0.9 4区 化学
Russian Journal of General Chemistry Pub Date : 2025-03-27 DOI: 10.1134/S1070363225600365
S. A. Znoiko, M. S. Kuz’mina, E. E. Molchanov, V. E. Maizlish, G. N. Koshel, N. V. Lebedeva
{"title":"Synthesis and Properties of Phthalonitriles with 2-Phenylphenoxy Groups and Corresponding Metallophthalocyanines","authors":"S. A. Znoiko,&nbsp;M. S. Kuz’mina,&nbsp;E. E. Molchanov,&nbsp;V. E. Maizlish,&nbsp;G. N. Koshel,&nbsp;N. V. Lebedeva","doi":"10.1134/S1070363225600365","DOIUrl":"10.1134/S1070363225600365","url":null,"abstract":"<p>4-(2-Phenylphenoxy)-5-nitro- and 4,5-di(2-phenylphenoxy)phthalonitriles were obtained by the reaction of 4-bromo-5-nitrophthalonitrile with 2-phenylphenol. Tetramerization of these precursors with acetates of selected divalent metals led to the synthesis of the corresponding octasubstituted phthalocyanines. Their spectral properties were investigated.</p>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"95 3","pages":"748 - 756"},"PeriodicalIF":0.9,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143716791","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}
引用次数: 0
Ultrasound-Promoted Ferrite Catalyzed One-Pot Multicomponent Synthesis of 3,4-Disubstituted Isoxazole-5(4H)-one Derivatives in Water as a Green Solvent with Evaluation of Antimicrobial Activity 超声促进铁氧体催化一锅多组分水中合成3,4-二取代异恶唑-5(4H)- 1衍生物及其抗菌活性评价
IF 0.9 4区 化学
Russian Journal of General Chemistry Pub Date : 2025-03-27 DOI: 10.1134/S1070363224613085
S. S. Ghevade, S. B. Kamble, K. N. Patil, V. S. Ingale, D. A. Kumbhar
{"title":"Ultrasound-Promoted Ferrite Catalyzed One-Pot Multicomponent Synthesis of 3,4-Disubstituted Isoxazole-5(4H)-one Derivatives in Water as a Green Solvent with Evaluation of Antimicrobial Activity","authors":"S. S. Ghevade,&nbsp;S. B. Kamble,&nbsp;K. N. Patil,&nbsp;V. S. Ingale,&nbsp;D. A. Kumbhar","doi":"10.1134/S1070363224613085","DOIUrl":"10.1134/S1070363224613085","url":null,"abstract":"<p>A systematic and efficient green method for the synthesis of advanced derivatives of isoxazole at room temperature was developed using ferrite as a catalyst. This process involves a simple one-pot multicomponent reaction of aromatic aldehydes, ethyl acetoacetate and hydroxylamine in a green solvent. The reaction time was significantly reduced by employing ultrasonic waves as an energy source. Key features of this protocol include a straightforward workup procedure, mild reaction conditions, the use of a green solvent, reusability of the catalyst and a developed synthesis that eliminates the need for purification steps such as chromatography.</p>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"95 3","pages":"671 - 678"},"PeriodicalIF":0.9,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143716925","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}
引用次数: 0
Fabrication of a BiVO4/CuCo2O4 Heterojunction Photoanode for Photoelectrochemical Water Splitting 用于光电化学水分解的BiVO4/CuCo2O4异质结光阳极的制备
IF 0.9 4区 化学
Russian Journal of General Chemistry Pub Date : 2025-03-27 DOI: 10.1134/S1070363224612018
D. Wenfei, X. Yonglei
{"title":"Fabrication of a BiVO4/CuCo2O4 Heterojunction Photoanode for Photoelectrochemical Water Splitting","authors":"D. Wenfei,&nbsp;X. Yonglei","doi":"10.1134/S1070363224612018","DOIUrl":"10.1134/S1070363224612018","url":null,"abstract":"<p>Bismuth vanadate (BiVO<sub>4</sub>) is highly studied for its potential in photoelectrochemical (PEC) water splitting, but its effectiveness is reduced by the rapid recombination of photogenerated carriers on the surface. This study presents a straightforward approach to integrating CuCo<sub>2</sub>O<sub>4</sub> with BiVO<sub>4</sub> to form a <i>p</i>–<i>n</i> junction, substantially enhancing the separation of electron-hole pairs on electrode surfaces. The photoelectrode BiVO<sub>4</sub>/CuCo<sub>2</sub>O<sub>4</sub>, which was prepared with an optimal CuCo<sub>2</sub>O<sub>4</sub> loading, achieved a significant photocurrent density of 1.26 mA/cm<sup>2</sup> at a potential of 1.23 V relative to the reversible hydrogen electrode (RHE). Experimental investigations confirmed that the presence of CuCo<sub>2</sub>O<sub>4</sub> enhances the mobility and separation of photogenerated electron-hole pairs. The outstanding performance in PEC water splitting demonstrated by the CuCo<sub>2</sub>O<sub>4</sub>/BiVO<sub>4</sub> composite electrode suggests its excellent suitability for applications involving solar-assisted water splitting.</p>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"95 3","pages":"572 - 579"},"PeriodicalIF":0.9,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143716668","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}
引用次数: 0
Design, Synthesis, Antibacterial, and Antifungal Activity Evaluation of 1,3,4-Oxadiazole Thioether Derivatives Incorporating a Methylsulfonyl Moiety 含有甲基磺酰基的1,3,4-恶二唑硫醚衍生物的设计、合成、抗菌和抗真菌活性评价
IF 0.9 4区 化学
Russian Journal of General Chemistry Pub Date : 2025-03-27 DOI: 10.1134/S1070363225600201
X.-S. Ran, P. Li, Q. Liu, F.-M. Zhang, D. Wang, W.-T. Mei, X. Wang
{"title":"Design, Synthesis, Antibacterial, and Antifungal Activity Evaluation of 1,3,4-Oxadiazole Thioether Derivatives Incorporating a Methylsulfonyl Moiety","authors":"X.-S. Ran,&nbsp;P. Li,&nbsp;Q. Liu,&nbsp;F.-M. Zhang,&nbsp;D. Wang,&nbsp;W.-T. Mei,&nbsp;X. Wang","doi":"10.1134/S1070363225600201","DOIUrl":"10.1134/S1070363225600201","url":null,"abstract":"<p>In this study, a series of novel 1,3,4-oxadiazole thioether derivatives incorporating a methylsulfonyl moiety were synthesized and their structures were characterized by <sup>1</sup>H, <sup>13</sup>C NMR, and HRMS. Bioassay results demonstrated that the target compounds exhibited moderate to good in vitro antibacterial activities against <i>Xanthomonas oryzae</i> pv. <i>oryzae</i> (<i>Xoo</i>), <i>Xanthomonas axonopodis</i> pv. <i>citri</i> (<i>Xac</i>), and <i>Wickerhamomyces anomalus</i> (<i>Wa</i>). Notably, 2-[(4-fluorobenzyl)thio]-5-[4-(methylsulfonyl)phenyl]-1,3,4-oxadiazole showed excellent antibacterial activities against these pathogens at concentrations of 200 and 100 μg/mL, with inhibition rates of 90 and 76% for <i>Xoo</i>, 84 and 64% for <i>Xac</i>, and 96 and 81% for <i>Wa</i>, respectively, which were even better than thiodiazole copper. However, the target compounds exhibited certain in vitro antifungal activities against <i>Penicillium sumatraense</i> (<i>Ps</i>) and <i>Aspergillus fumigatus</i> (<i>Af</i>) at 50 μg/mL, with the inhibition rates of 25–46 and 18–42%, respectively, which were lower than those of prochloraz. To the best of our knowledge, it is the first report on the synthesis and bioactivity evaluation of this series of 1,3,4-oxadiazole thioether derivatives incorporating a methylsulfonyl moiety.</p>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"95 3","pages":"742 - 747"},"PeriodicalIF":0.9,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143716790","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}
引用次数: 0
Design, Synthesis, and Bioactivity Evaluation of Novel Sulfone Derivatives Incorporating an 1,2,4-Triazole Moiety 新型含1,2,4-三唑砜衍生物的设计、合成及生物活性评价
IF 0.9 4区 化学
Russian Journal of General Chemistry Pub Date : 2025-03-27 DOI: 10.1134/S107036322560050X
J. Liu, C. He, B. Tan, W. Wu, L. Yu, P. Li
{"title":"Design, Synthesis, and Bioactivity Evaluation of Novel Sulfone Derivatives Incorporating an 1,2,4-Triazole Moiety","authors":"J. Liu,&nbsp;C. He,&nbsp;B. Tan,&nbsp;W. Wu,&nbsp;L. Yu,&nbsp;P. Li","doi":"10.1134/S107036322560050X","DOIUrl":"10.1134/S107036322560050X","url":null,"abstract":"<p>Herein, a series of novel sulfone derivatives incorporating an 1,2,4-triazole moiety was synthesized and their structures were confirmed by <sup>1</sup>H NMR, <sup>13</sup>C NMR, and HRMS. The in vitro antibacterial activities of these compounds against <i>Wickerhamomyces anomalus</i> (<i>Wa</i>) and <i>Bacillus cereus</i> (<i>Bc</i>) at concentrations of 200 and 100 μg/mL were evaluated using the turbidimeter tests. The results demonstrated that the target compounds exhibited moderate to good antibacterial activities against <i>Wa</i> and <i>Bc</i>. Notably, 3-{[(4-chlorophenyl)sulfonyl]methyl}-5-[(4-fluorobenzyl)thio]-4-methyl-4<i>H</i>-1,2,4-triazole showed excellent in vitro antibacterial activity against <i>Bc</i> at 200 μg/mL, with a 100% inhibition rate. Additionally, the in vitro antifungal activities of these compounds against <i>Penicillium sumatraense</i> (<i>Ps</i>) and <i>Aspergillus fumigatus</i> (<i>Af</i>) were assessed using the mycelium growth rate method. Bioassay results indicated that the target compounds exhibited certain antifungal activities against <i>Ps</i> and <i>Af</i> at 50 μg/mL. Specifically, 3-{[(4-chlorophenyl)sulfonyl]methyl}-4-phenyl-5-(propylthio)-4<i>H</i>-1,2,4-triazole displayed moderate antifungal activity against <i>Ps</i> at 50 μg/mL, with an inhibition rate of 64.52%. To the best of our knowledge, this study is the first to report on the synthesis and bioactivity evaluation of this series of novel sulfone derivatives incorporating an 1,2,4-triazole moiety.</p>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"95 3","pages":"757 - 763"},"PeriodicalIF":0.9,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143716792","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}
引用次数: 0
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