Journal of Heterocyclic Chemistry最新文献_第7页

Transition-Metal-Free C-1 Arylation of Isoquinolines With Arylhydrazine Salts 异喹啉类与芳酰肼盐的无过渡金属C-1芳基化

IF 2 3区化学

Journal of Heterocyclic Chemistry Pub Date : 2026-04-05 Epub Date: 2026-02-02 DOI: 10.1002/jhet.70168

Xing Wang, Caifu Deng, Yongdong Yang, Aibo Liu, Shenggang Yang, Rong Tan, Ling Li, Lei Tang, Cong Wang

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Advancement in the Synthesis of N-Substituted Phenothiazines n取代吩噻嗪类化合物的合成研究进展

IF 2 3区化学

Journal of Heterocyclic Chemistry Pub Date : 2026-04-05 Epub Date: 2026-01-20 DOI: 10.1002/jhet.70163

Ishika Taliyan, Khushbu Upadhyay, Shruti, Jaya Dwivedi

{"title":"Advancement in the Synthesis of N-Substituted Phenothiazines","authors":"Ishika Taliyan, Khushbu Upadhyay,  Shruti, Jaya Dwivedi","doi":"10.1002/jhet.70163","DOIUrl":"https://doi.org/10.1002/jhet.70163","url":null,"abstract":"<div>\u0000 \u0000 N-substituted phenothiazine derivatives are useful heterocycles that are known to have diverse uses in therapeutic agents, electronic devices, and as materials. Earlier approaches for the synthesis of N-substituted phenothiazines are based on nucleophilic substitution, amine coupling, and other routine organic transformations, which frequently require the utilization of environmentally damaging solvents/agents. The appearance of green chemistry has given rise to another synthetic strategy that aims to avoid the use of hazardous substances and to maximize yield. The green approach has various advantages, including time saving, less usage of solvents, and improved yields. Specifically, microwave-induced reactions and solvent-free systems provide higher energy efficiency and purity of the final product. Further, new catalytic methods via green rhodium and palladium catalysts, along with the green solvent Deep Eutectic Solvents, are shown for the synthesis of complex N-substituted phenothiazine derivatives, including the functionalized forms to improve electron transport and photostability, which are beneficial in the application of the materials. This review seeks to present conventional and green synthetic methodologies for the synthesis of N-substituted phenothiazine and to point out both the advantages and disadvantages of each; also, to showcase the possible impact of greener advances for the sustainable synthesis of these multifunctional compounds.\u0000 </div>","PeriodicalId":194,"journal":{"name":"Journal of Heterocyclic Chemistry","volume":"63 4","pages":"670-702"},"PeriodicalIF":2.0,"publicationDate":"2026-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147668691","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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Indole-Based π-Extended Monophosphine Ligands for Enhanced Palladium-Catalyzed Sonogashira Coupling 吲哚基π扩展单膦配体增强钯催化Sonogashira偶联

IF 2 3区化学

Journal of Heterocyclic Chemistry Pub Date : 2026-04-05 Epub Date: 2026-02-04 DOI: 10.1002/jhet.70151

Yu Kiu Lau, Chun Pong Hui, Cheuk Long Li, Ho Chung Chang, Man Ho Tse, Ho Kwan Lou, Iat In Chan, Raymond Wai-Yin Sun, Pui Ying Choy, Fuk Yee Kwong

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An Efficient Practicable Synthesis of 2,4-Disubstituted Imidazole Derivatives Using Dual Functions of Deep Eutectic Solvent (DES) 利用深度共晶溶剂双功能高效合成2,4-二取代咪唑衍生物

IF 2 3区化学

Journal of Heterocyclic Chemistry Pub Date : 2026-04-05 Epub Date: 2026-02-06 DOI: 10.1002/jhet.70169

Sanshay Sen, Sudip Mondal, Kousik Giri, Adinath Majee

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In-Demand and Now Available: N-Difluoromethylpyrazoles 需求和现有供应：n-二氟甲基吡唑

IF 2 3区化学

Journal of Heterocyclic Chemistry Pub Date : 2026-04-05 Epub Date: 2026-01-26 DOI: 10.1002/jhet.70167

Bogdan Ugrak, Tatyana Dutova, Vyacheslav Rusak, Evgeny Tretyakov

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Lewis Acid–Catalyzed Annulation of 2(Trifluoroacetyl)pyrroles Leading to CF3-Substituted Polycyclic Quinazolinones Lewis酸催化2（三氟乙酰基）吡咯环化生成cf3取代的多环喹唑啉酮

IF 2 3区化学

Journal of Heterocyclic Chemistry Pub Date : 2026-04-05 Epub Date: 2026-02-03 DOI: 10.1002/jhet.70166

Karumanchi Susmitha, Akuthota Thulasi, Neelam Yugandhar Sreedhar

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Potential Anticancer Agents Based on Monoterpenic Skeleton With Mono and Bis-Isoxazoline Derivatives: Diastereoselective Synthesis, Experimental Study, Evaluation of Biological Activity, and Molecular Docking 基于单萜烯骨架和单、双异恶唑啉衍生物的潜在抗癌药物：非对映选择性合成、实验研究、生物活性评价和分子对接

IF 2 3区化学

Journal of Heterocyclic Chemistry Pub Date : 2026-04-05 Epub Date: 2026-01-04 DOI: 10.1002/jhet.70158

Abdoullah Bimoussa, Abdellah N’Ait Ousidi, Mourad Fawzi, Az-Eddine El Mansouri, Yassine Laamari, Ali Oubella, Aziz Auhmani, Rabiaa Fdil, Hamid Morjani, Anthony Robert, Abdelkhalek Riahi, Jean-Claude Daran, Moulay Youssef Ait Itto

{"title":"Potential Anticancer Agents Based on Monoterpenic Skeleton With Mono and Bis-Isoxazoline Derivatives: Diastereoselective Synthesis, Experimental Study, Evaluation of Biological Activity, and Molecular Docking","authors":"Abdoullah Bimoussa, Abdellah N’Ait Ousidi, Mourad Fawzi, Az-Eddine El Mansouri, Yassine Laamari, Ali Oubella, Aziz Auhmani, Rabiaa Fdil, Hamid Morjani, Anthony Robert, Abdelkhalek Riahi, Jean-Claude Daran, Moulay Youssef Ait Itto","doi":"10.1002/jhet.70158","DOIUrl":"https://doi.org/10.1002/jhet.70158","url":null,"abstract":"<div>\u0000 \u0000 A facile synthesis of fused isoxazolines has been carried out using a 1,3-dipolar cycloaddition reaction of arylonitrile oxides on (R)-Carvone under different stoichiometry conditions. The newly synthesized compounds were fully characterized via spectroscopic analysis and then evaluated for their in vitro antiproliferative properties against four cancer cell lines, namely HT1080, MCF-7, MDA-MB-231, and A-549. All the mono-isoxazolines showed low cytotoxicity (> 100 μM) and the large majority of bis-isoxazolines revealed moderate antiproliferative activity. The derivative 11b was the most potent one against HT-1080 and MDA-MB-231 with respective IC50 values of 14.85 and 15.37 μM. A comprehensive study also showed that bis-isoxazoline 11b induced apoptosis involving a mitochondria-mediated signaling pathway and cell cycle arrest at the G0/G1 phase for HT-1080 and G2/M for MDA-MB-231. Finally, compound 11b showed a high binding affinity in the molecular docking study at the binding pockets of the Caspase-3 and Bcl-2 proteins, consistent with the results of biological experiments. Furthermore, this anticancer activity may be triggered by binding to active sites of caspase-3 and Bcl-2.\u0000 </div>","PeriodicalId":194,"journal":{"name":"Journal of Heterocyclic Chemistry","volume":"63 4","pages":"590-606"},"PeriodicalIF":2.0,"publicationDate":"2026-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147668003","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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Design, Synthesis, and Biological Evaluation of Some New Thiazole-Based Compounds as Antioxidant and Antimicrobial Agents 一些新型噻唑类抗氧化和抗菌化合物的设计、合成及生物学评价

IF 2 3区化学

Journal of Heterocyclic Chemistry Pub Date : 2026-04-05 Epub Date: 2025-12-30 DOI: 10.1002/jhet.70155

Fatima S. Mehdhar, Ehab Abdel-Latif, Ebrahim Abdel-Galil, Ghada E. Abdel-Ghani

{"title":"Design, Synthesis, and Biological Evaluation of Some New Thiazole-Based Compounds as Antioxidant and Antimicrobial Agents","authors":"Fatima S. Mehdhar, Ehab Abdel-Latif, Ebrahim Abdel-Galil, Ghada E. Abdel-Ghani","doi":"10.1002/jhet.70155","DOIUrl":"https://doi.org/10.1002/jhet.70155","url":null,"abstract":"<div>\u0000 \u0000 This work aims to synthesize novel thiazole analogues through a strategic multicomponent reaction connecting ethyl 2-(2-aminothiazol-4-yl)acetate (1). The acetohydrazide derivative 2 is chloroacetylated twice: at the amino and acetohydrazide groups. Reacting the conforming bis-chloroacetamide derivative 3 with two molar values of 2-mercaptobenzothiazole resulted in the equivalent bissulfide compound 4. The base-catalyzed addition of thiazole derivative 1 to phenyl isothiocyanate afforded intermediate 5, which upon subsequent reaction with ethyl bromoacetate yielded the corresponding thiazolyl-thiazolidine derivative 6. The heated chloroacetamide 7 with ammoniumthio cyanate to give thiazolidin-4-one hybrid 9 was condensed with 3 aromatic aldehyde derivatives furnishing the corresponding 5-arylidene-2-imino-4-thiazolidinones 10a–c, also the synthesized compound 7 was treated with two kinds of thiocarbamoyl compounds 11 and 13 to produce thiazolylthiophenes 12 and 14. Comprehensive structural characterization of the novel synthesized analogues was achieved using elemental analysis and characterized using 1H NMR, 13C NMR, FT-IR, and ESI-MS spectroscopy. The designed thiazole-based compounds exhibited broad-spectrum against antioxidant and antimicrobial activities which will facilitate their rational usage in multiple therapeutic applications.\u0000 </div>","PeriodicalId":194,"journal":{"name":"Journal of Heterocyclic Chemistry","volume":"63 4","pages":"567-578"},"PeriodicalIF":2.0,"publicationDate":"2026-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147668913","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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Recent Advances in the Synthesis of Biologically and Pharmaceutically Active Thiazole and Its Analogues 生物和药物活性噻唑及其类似物的合成研究进展

IF 2 3区化学

Journal of Heterocyclic Chemistry Pub Date : 2026-04-05 Epub Date: 2026-02-11 DOI: 10.1002/jhet.70170

Khushbu Upadhyaya, Shruti, Rekha Sharma, Jaya Dwivedi

{"title":"Recent Advances in the Synthesis of Biologically and Pharmaceutically Active Thiazole and Its Analogues","authors":"Khushbu Upadhyaya,  Shruti, Rekha Sharma, Jaya Dwivedi","doi":"10.1002/jhet.70170","DOIUrl":"https://doi.org/10.1002/jhet.70170","url":null,"abstract":"<div>\u0000 \u0000 Recently, thiazoles have become essential heterocyclic compounds owing to their versatile applications in various fields. It also plays a major role in the pharmaceutical industry and is a critical scaffold for drug discovery. There are currently a lot of articles reporting the synthesis and functionalization of biological and pharmaceutical functions. To date, a variety of synthesis protocols for scaffold construction have been mentioned in the literature. For instance, classical synthesis protocols like Hantzsch synthesis, Cook-Heilbron synthesis, and Gabriel synthesis have been used to build the main thiazole scaffold. Ultrasound irradiation reactions, microwave-assisted and green reaction protocols are also useful for building and functionalizing this compound. This review's main objective is to draw attention to the synthesis techniques and discoveries that were previously discussed in order to address the drawbacks of synthesis and their environmental effect. In addition, various selected thiazoles and their derivatives with potential biological and pharmaceutical activities will be discussed.\u0000 </div>","PeriodicalId":194,"journal":{"name":"Journal of Heterocyclic Chemistry","volume":"63 4","pages":"748-772"},"PeriodicalIF":2.0,"publicationDate":"2026-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147668379","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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IF 2 3区化学

Journal of Heterocyclic Chemistry Pub Date : 2026-03-05

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