Article
Chemistry, Multidisciplinary
Yifan Cui, Yizhan Zhai, Junzhe Xiao, Can Li, Wei-Feng Zheng, Chaofan Huang, Guolin Wu, Anni Qin, Jie Lin, Qi Liu, Huanan Wang, Penglin Wu, Haibo Xu, Yangguangyan Zheng, Shengming Ma
Summary: The article discusses the creation and reaction of axial chirality memory, achieving highly stereoselective reactions using an optically active alkylidene-pi-allyl iridium intermediate. This method shows compatibility with substituents on both amines and 2,3-allenyl carbonates with high efficiency, while mechanistic experiments reveal slow isomerization rates.
Article
Chemistry, Organic
Kailu Li, Qianmin Li, Qinhao Shi, Yanmin He, Wenquan Yu, Junbiao Chang
Summary: An iodine-mediated direct sp(3) C-H amination reaction has been developed for the synthesis of nitrogen-containing compounds from readily available substrates under transition-metal-free conditions. This method is operationally simple and can be conveniently conducted on a large scale under mild reaction conditions.
ASIAN JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Physical
Hiroki Miura, Tomoya Toyomasu, Hidenori Nishio, Tetsuya Shishido
Summary: A gold-catalyzed thioetherification of C(sp(3))-O bonds is reported, using allyl phosphates and thiosilanes as substrates. The reaction proceeds efficiently under mild conditions, providing the corresponding allyl sulfides with excellent yields. The study also demonstrates the thioetherification of C-O bonds in benzyl and propargyl phosphates, as well as the high enantiomeric purity achieved in the reaction of an optically active benzyl phosphate. Soluble gold species are identified as the responsible catalysts, with cationic gold species on ZrO2-supported gold nanoparticles serving as the active catalytic species.
CATALYSIS SCIENCE & TECHNOLOGY
(2022)
Article
Chemistry, Organic
Jinyuan Jiang, Jidan Liu, Zhenke Yang, Jieying Zheng, Xin Tian, Liyao Zheng, Zhao-Qing Liu
Summary: An efficient method has been developed for the direct C-H oxidative annulation of isoquinolones with allyl alcohols, leading to the synthesis of structurally diverse isoindolo[2,1-b]isoquinolin-5(7H)-ones with high atom economy. This protocol is tolerant of a broad spectrum of functionalities and can be conducted in one-pot operation using readily available N-methoxybenzamides.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2022)
Article
Chemistry, Organic
Yan Zheng, Siqi Dong, Kai Xu, Delong Liu, Wanbin Zhang
Summary: An efficient Pd-catalyzed asymmetric allylic substitution cascade reaction has been developed for the synthesis of chiral compounds. The reaction achieved high yields and high enantioselectivity under temperature-controlled conditions, and can be performed on a gram scale. The resulting product is versatile and can undergo various transformations.
Article
Chemistry, Multidisciplinary
Vinayak Hanchate, Sudharshan Nagabhushana Reddy, Anil Kumar, Kandikere Ramaiah Prabhu
Summary: The reactivity of sulfoxonium ylide with allyl carbonates and allyl carbamates diverges. Rh(iii)-catalyzed C-H activation and cyclization of sulfoxonium ylide with ally esters leads to the formation of a cyclopropane-fused tetralone derivative via cascade C-H activation, (4+2) annulation, and cyclopropanation. A similar reaction of sulfoxonium ylide with allyl carbamates forms a C3-substituted indanone derivative through a rare and interesting domino C-H activation and (4+1) annulation in which allyl carbamate acts as a C1-synthon.
CHEMICAL COMMUNICATIONS
(2023)
Article
Chemistry, Multidisciplinary
Dhananjay S. Nipate, Neha Meena, Prakash N. Swami, Krishnan Rangan, Anil Kumar
Summary: In this study, the synthesis of functionalized benzo[a]phenazines and indazolo[2,3-a]quinolines was achieved through Rh(III)-catalyzed oxidative annulation of 2-arylquinoxalines and 2-aryl-2H-indazoles with allyl alcohols. The method showed a wide substrate scope, excellent functional group tolerance, good to high yields of annulated products, and the capability for scaled-up synthesis. A tentative mechanism of the annulation reaction was proposed based on a preliminary mechanistic investigation.
CHEMICAL COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Soya Ishikawa, Ryo Togashi, Ryosuke Ueda, Shunsuke Onodera, Takuya Kochi, Fumitoshi Kakiuchi
Summary: In this paper, a highly efficient deallylative beta-acylalkylation reaction of allylbenzene derivatives with allyl alcohols in the presence of Cp*Rh catalysts is reported. It was found that allylbenzene derivatives possessing pyridyl and pyrazolyl directing groups can be converted to beta-aryl ketones via cleavage of C(aryl)-C(allyl) bonds. Furthermore, synthesis of a quinoline derivative from a beta-aryl ketone product bearing a pyrazolyl group was also achieved.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Editorial Material
Chemistry, Multidisciplinary
Bao-Le Qu, Mao-Mao Zhang, Liang-Qiu Lu, Wen-Jing Xiao
Summary: The study presents an iridium-catalyzed reaction for asymmetric synthesis of Z-allyl esters, allowing for the elegant preparation of important chiral Z-olefins.
Article
Chemistry, Multidisciplinary
Yasuhiro Yamashita, Io Sato, Ryota Fukuyama, Shu Kobayashi
Summary: Catalytic imino-ene-type allylation reactions of unactivated allyl compounds were achieved using a catalytic amount of a strongly basic mixed system. The reactions proceeded smoothly at low temperature, and notably, the gaseous alkene propylene could be used in this system.
CHEMICAL COMMUNICATIONS
(2022)
Article
Chemistry, Organic
Xiaodong Xiong, Jonathan Wong, Ying-Yeung Yeung
Summary: A facile, efficient, and chemoselective synthesis of allylic amides has been developed using allyl bromides activated by silver triflate. The Ritter-type reaction readily proceeds under mild conditions to give various allyl amides. This protocol is also applicable to different nucleophilic partners to yield a wide range of allyl-substituted products in the absence of a base.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Joshua C. DeMuth, Zhihui Song, Stephanie H. Carpenter, Theresa E. Boddie, Aleksa Radovic, Tessa M. Baker, Osvaldo Gutierrez, Michael L. Neidig
Summary: The study investigates the reaction mechanisms of iron-catalysed C-H allylation and C-H amination systems. Through spectroscopic and kinetic analysis, a rapid reaction pathway between the iron-activated intermediate and the electrophile is revealed. The results provide critical insights for the rational design and development of improved C-H functionalisation systems.
Article
Chemistry, Organic
Rina Muto, Kenji Nagata, Yoshiki Nakazumi, Kaho Nakamura, Satoshi Ueno
Summary: The Pd/PMe3-catalyzed allylation reaction of 1-(cyanomethyl)naphthalenes with allyl acetates showed para-selectivity instead of aregioselectivity. This reaction proceeds through ligand attack on the para-carbon of the arenes, which is electronically enriched by a cyano-stabilized α-carbanion. This leads to the formation of (p-allyl)palladium intermediate and a 1,5-hydrogen shift of the parahydrogen.
Article
Chemistry, Applied
Marcos San Segundo, Arkaitz Correa
Summary: This study describes a radical alpha-C-H alkylation of a collection of N-picolinamide amino acid derivatives using ethers and cycloalkanes as chemical feedstock. This method is characterized by its reliable scalability and removable auxiliary group, and allows for the assembly of various tri- and tetrasubstituted amino acid compounds.
ADVANCED SYNTHESIS & CATALYSIS
(2022)
Article
Chemistry, Organic
Jianpeng Chen, Yu Tang, Biao Yu
Summary: A mild glycosylation method using glycosyl 1-methylimidazole-2-carboxylates has been developed, with the reaction being promoted by metal triflates and triflimides, especially Cu(OTf)(2). The reaction is initiated by coordination of the glycosyl ester donor with the metal cation assisted by the adjacent 1-methylimidazole chelating group.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Gaurav Gopal Naik, Ankit Uniyal, Deepak Chouhan, Vinod Tiwari, Alakh N. Sahu
Summary: This review discusses the potential of various natural molecules, such as capsaicinoids and curcumin, to activate TRPV1 channels and be used for the treatment of neuropathic pain.
CURRENT PHARMACEUTICAL BIOTECHNOLOGY
(2022)
Article
Multidisciplinary Sciences
Komal Singh, Rajesh Kumar, Fareha Umam, Prerna Kapoor, Sudhir Sinha, Amita Aggarwal
Summary: This study identifies B cell responses that distinguish between latent tuberculosis infection (LTBI) and active TB disease. The results suggest that the ratio of IgM to IgG antibodies, antibody binding to specific antigens, and the frequency of memory B cell subsets could indicate the protective or pathogenic immune responses following primary infection with Mycobacterium tuberculosis (Mtb).
Article
Computer Science, Software Engineering
Prabhakar N. N. Kota, Ashok S. S. Chandak, B. P. Patil
Summary: Industrial 4.0 makes manufacturers more vulnerable to current challenges and makes it easier to adapt to market changes. The research aims to overcome the issues of information security and control systems by developing a hybrid machine learning technique. The experimental results show that the proposed technique performs well in various metrics.
CONCURRENCY AND COMPUTATION-PRACTICE & EXPERIENCE
(2023)
Review
Nanoscience & Nanotechnology
Saurabh Shah, Paras Famta, Vinod Tiwari, Arun K. Kotha, Rama Kashikar, Mahavir Bhupal Chougule, Young Hun Chung, Nicole F. Steinmetz, Mohammad Uddin, Shashi Bala Singh, Saurabh Srivastava
Summary: This article reviews and discusses the interplay between tumor microenvironment and the immunological cascade and how it can be utilized to develop nanoparticle-based cancer vaccines and immunotherapies. Nanoparticles and proteinaceous vaccines have enormous potential in cancer therapy.
WILEY INTERDISCIPLINARY REVIEWS-NANOMEDICINE AND NANOBIOTECHNOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Priyanka Bose, Manoj K. Jaiswal, Sumit K. Singh, Rakesh K. Singh, Vinod K. Tiwari
Summary: In nature, glycan chains called sialic acids or nuraminic acids cover most cells and have long been recognized for their therapeutic importance. Sialic acid-containing glycans play a crucial role on cell surfaces, modulating and mediating various cellular interactions. Understanding the interaction between sialo-proteins and their roles in vertebrates has had a significant impact on medicine.
CARBOHYDRATE RESEARCH
(2023)
Article
Pharmacology & Pharmacy
Shivani Jaiswal, Vinod Akhilesh, Vinod Tiwari, Senthil Raja Ayyannan
Summary: The isatin-derived carbohydrazone, SIH 3, showed significant anti-nociceptive activity in the neuropathic pain model without altering locomotor activity. It also displayed excellent safety profile in acute oral toxicity study and exhibited antioxidant effect in oxidative stress induced by chronic constrictive injury.
PHARMACOLOGICAL REPORTS
(2023)
Article
Chemistry, Organic
Sunil Kumar, Mangal S. Yadav, Sumit K. Singh, Sanchayita Rajkhowa, Vinod K. Tiwari
Summary: A modular and reliable click approach was used to synthesize lactose- and galactose-coated calixarenecored G(1) and G(2) generation glycodendrimers efficiently. The characterization of the developed calixarene glycodendrimers was performed using extensive spectral analysis including NMR (H-1 and C-13), MS, IR, and SEC data.
Article
Biochemistry & Molecular Biology
Priyanka Bose, Anand K. Agrahari, Rajan Singh, Mala Singh, Sunil Kumar, Rakesh K. Singh, Vinod K. Tiwari
Summary: A click-inspired piperazine glycoconjugate was developed to synthesize water-soluble and biocompatible motifs. This study focused on designing and synthesizing versatile sugar-appended triazoles using "Click Chemistry", and evaluated their pharmacological properties on cyclin-dependent kinases (CDKs) and cytotoxicity on cancer cells through in silico and in vitro approaches, respectively. The galactose- and mannose-derived piperazine conjugates were identified as promising motifs. The galactosyl bis-triazolyl piperazine analogue 10b was found to be the most interactive with CDKs and showed significant anticancer activity.
CARBOHYDRATE RESEARCH
(2023)
Review
Chemistry, Multidisciplinary
Manoj K. Jaiswal, Vinod K. Tiwari
Summary: Click Chemistry is a modular, rapid, and reliable tool used for the regioselective 1,2,3-triazole forming [3+2] reaction of organic azide and terminal alkyne. It is widely explored in various emerging research domains. The intramolecular click chemistry, which involves metal-catalyzed cyclization, organo-catalyzed cyclization, and thermal-induced topochemical reaction, is less addressed compared to the intermolecular metal variant. Recent approaches on intramolecular azide-alkyne cycloaddition 'Click Chemistry' and their emerging applications in the development of diverse molecules are reported.
Article
Chemistry, Multidisciplinary
Manoj K. Jaiswal, Abhishek Gupta, Mangal S. Yadav, Vinay K. Pandey, Vinod K. Tiwari
Summary: A novel organocatalyzed [3+2] cycloaddition reaction has been developed for the construction of 1,5-disubstituted triazolyl glycoconjugates. The reaction involves the use of Schreiner thiourea organocatalysts to activate nitroolefins through double hydrogen bonding. This metal-free and acid-free synthetic protocol is operationally simple, regioselective, and complements the classical RuAAC catalyzed synthesis of 1,5-disubstituted 1,2,3-triazoles. By using catalytic amounts of the Schreiner thiourea organocatalyst, a wide range of organic azides can react with nitroolefins to produce diverse 1,5-disubstituted 1,2,3-triazoles in good yields with excellent regioselectivity.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Organic
Sumit K. Singh, Sunil Kumar, Mangal S. Yadav, Abhishek Gupta, Vinod K. Tiwari
Summary: This report describes a convenient method for the Cu(I)-catalyzed Sonogashira cross-coupling reaction of aryl/heteroaryl halides and alkynyl sugars using a glycohybrid ligand. The method has notable features, including low catalytic loading, cost-effectiveness, and a wide substrate scope.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Organic
Sumit K. Singh, Sunil Kumar, Mangal S. Yadav, Subrato Bhattacharya, Vinod K. Tiwari
Summary: This report describes a convenient Cu(I)-catalyzed tandem synthesis method for the efficient synthesis of dihydrophenanthridinediones and substituted isoquinolinones using glycosyl 1,2,3-triazole-based pyridinamide ligands. The method successfully forms biologically relevant heterocyclic scaffolds in high yields through intermolecular C-C cross-coupling followed by intramolecular cyclization. Notable features of this method include low catalytic loading, use of cost-effective and biocompatible ligands, high reaction yield, and easily accessible starting materials, making it a versatile protocol.
SYNTHESIS-STUTTGART
(2023)
Review
Chemistry, Organic
Mangal S. Yadav, Abhishek Gupta, Priyanka Bose, Anoop S. Singh, Prabhu P. Mohapatra, Vinod K. Tiwari
Summary: N-Acylbenzotriazoles are important synthons in organic synthesis and can serve as alternative acylating agents in various organic transformations. This review summarizes the preparation methods of N-Acylbenzotriazole derivatives and their diverse applications, highlighting their ability to conveniently synthesize biologically important organic compounds as alternative acylating agents. The significance of using benzotriazole ring cleavage methodology in compound synthesis is also emphasized.
Article
Engineering, Electrical & Electronic
Pravin Balaso Chopade, Prabhakar N. Kota, Bhagvat D. Jadhav, Pravin Marotrao Ghate, Shankar Dattatray Chavan
Summary: The ultimate goal of the Super-Resolution (SR) technique is to generate high-resolution images by combining low-resolution images. This technique has various applications such as surveillance, remote sensing, and medical diagnosis. However, existing reconstruction methods often suffer from artifacts such as noise and blurring. This research proposes a method to improve the effectiveness of SR image reconstruction by enhancing visual information and autonomous machine perception.
INTERNATIONAL JOURNAL OF ELECTRICAL AND COMPUTER ENGINEERING SYSTEMS
(2023)
Article
Multidisciplinary Sciences
Sudhir Sinha, Shashikant Kumar, Komal Singh, Fareha Umam, Vinita Agrawal, Amita Aggarwal, Barbara Imperiali
Summary: Styrene maleic acid lipid particles (SMALPs) were utilized to prepare and characterize membrane proteins of Mycobacterium tuberculosis (Mtb). These nanoparticles contained inner membrane protein PRA, membrane-associated proteins PstS1, LpqH and Ag85, and lipoglycan LAM. Peripheral membrane proteins Acr and PspA were excluded. Additionally, immune responses indicated that only MtM-SMALPs could induce the production of TNF-alpha.
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
