Article
Chemistry, Organic
Lihua Luo, Juan Tang, Rui Sun, Wenjing Li, Xueli Zheng, Maoling Yuan, Ruixiang Li, Hua Chen, Haiyan Fu
Summary: A direct and efficient synthesis method for sulfonyl iminopyridine derivatives has been developed, featuring the formation of a C-N bond with high functional group tolerance under metal-free conditions. The spectroscopic properties of these compounds have the potential to make them useful as new emitting materials.
Article
Chemistry, Multidisciplinary
Myojeong Kim, Euna You, Seongjin Park, Sungwoo Hong
Summary: The modern synthesis aims to develop distinct reaction pathways from identical starting materials for efficient synthesis of diverse compounds. By controlling the reaction conditions and using specific compound combinations, the method allows for high-efficiency synthesis of a variety of compounds with a broad substrate scope and mild reaction conditions.
Article
Polymer Science
Yang Lou, Jamie Gaitor, Megan Treichel, Kevin J. T. Noonan, Edmund F. Palermo
Summary: This study reports on a new type of antimicrobial polymer with unusually bulky tetraaminophosphonium groups, which act as highly delocalized cationic charges. These bulky cations significantly enhance the biocidal activity of amphiphilic polymers, resulting in potent antibacterial activity against E. coli. The flexibility of polymer chains and the spacer arm groups separating the cations from the backbone main chain have minimal effects on the activity. Counterion effects were observed, with tightly bound PF6- counteranions showing poor activity and loosely bound Cl- counterions exhibiting potent activity.
Review
Chemistry, Multidisciplinary
Jinjie Chang, Gang Zhao, Xinyuan Zhao, Chunlin He, Siping Pang, Jean'ne M. Shreeve
Summary: The article discusses the synthesis strategies for energetic iodine-rich compounds and the synthesis routes for oxygen-containing iodine-rich compounds to improve oxygen balance and achieve high-energy and high-iodine content. It also summarizes research on iodine-containing polymers.
ACCOUNTS OF CHEMICAL RESEARCH
(2021)
Article
Plant Sciences
Huynh Nguyen Khanh Tran, Min Jin Kim, A-Young Shin, Le Viet Ha Tran, Jihoon Lee, Yeon-Ju Lee
Summary: Ten new norterpene alkaloids, coscinoderines A-J (1-10), were isolated from the marine sponge Coscinoderma bakusi. Each coscinoderine contains a 1,2,5-trisubstituted pyridinium moiety bearing a terpene unit at the C-2 position. The structures were determined using NMR and HRMS data, and the absolute stereochemistry of compound 4 was confirmed by comparing calculated and measured ECD spectra. The discovery of these coscinoderines expands the range of pyridinium alkaloids found in marine sponges.
JOURNAL OF NATURAL PRODUCTS
(2023)
Article
Chemistry, Multidisciplinary
Wooseok Lee, Yejin Koo, Hoimin Jung, Sukbok Chang, Sungwoo Hong
Summary: Photocycloaddition is an efficient reaction that allows the conversion of alkenes into high-value synthetic materials under thermal conditions. In this study, a diastereoselective pyridyl lactamization was achieved through a photoinduced [3+2] cycloaddition using the reactivity of N-N pyridinium ylides, which can form triplet diradical intermediates and undergo stepwise radical cycloaddition with a broad range of alkenes. This method shows excellent efficiency, diastereoselectivity, and functional group tolerance, providing a useful synthon for the synthesis of ortho-pyridyl β- and δ-lactam scaffolds in a single step.
Article
Chemistry, Organic
Benjamin T. Boyle, J. Luke Koniarczyk, Andrew McNally
Summary: The N-phosphonium pyridinium intermediates exhibit unusual reactivity in pyridine SNAr reactions. The activation mode described in this study allows for ambient temperature C-P bond formation and is effective across a wide range of substrates.
Article
Biochemical Research Methods
Bradley M. Lipka, Vincent M. Betti, Daniel S. Honeycutt, Daniel L. Zelmanovich, Max Adamczyk, Ruojun Wu, Harrison S. Blume, Caitlin A. Mendina, Jacob M. Goldberg, Fang Wang
Summary: We present a series of fluorinated cationic reagents that enable rapid arylation of cysteine under mild conditions, resulting in high reaction rates and easy application. This method allows for the direct coupling of structurally diverse phenol-containing functional motifs to cysteine residues and has potential applications in various fields.
BIOCONJUGATE CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Melina S. Weber, Margit Schulze, Giuseppe Lazzara, Antonio Palumbo Piccionello, Andrea Pace, Ivana Pibiri
Summary: This study discusses the synthesis and characterization of a new class of 1,2,4-oxadiazolylpyridinium as a cationic scaffold for fluorinated ionic liquid crystals. A series of 12 fluorinated heterocyclic salts based on a 1,2,4-oxadiazole moiety, connected to an N-alkylpyridinium unit and a perfluoroheptyl chain, with different alkyl chain lengths and counterions, have been synthesized. The thermotropic properties of these salts, particularly the existence of an enantiotropic mesomorphic smectic liquid crystalline phase for six bis(trifluoromethane)sulfonimide salts, have been investigated.
APPLIED SCIENCES-BASEL
(2021)
Article
Electrochemistry
Nitaro Yuza, Nobuyuki Serizawa, Yasushi Katayama
Summary: The research investigated the anodic dissolution and electropolishing of Sn in an amide-type ionic liquid. It was found that the rate of anodic dissolution was determined by the diffusion of Sn(II) species. Through in-situ observation of a large increase in local viscosity, a shiny surface was obtained, and a decrease in surface roughness indicated that electropolishing of Sn was possible due to the formation of a viscous layer near the electrode.
JOURNAL OF THE ELECTROCHEMICAL SOCIETY
(2021)
Review
Oncology
M. Platten, L. Bunse, W. Wick
Summary: The development of anticancer vaccines has been hindered by a lack of suitable tumor-specific antigens, while IDH1R132H mutation generates a shared clonal neoepitope recognized by mutation-specific T-helper cells, providing new directions for certain cancer vaccines.
Article
Polymer Science
Mohamed H. El-Newehy, A. Meera Moydeen, Ali K. Aldalbahi, Badr M. Thamer, Yehia A. -G. Mahmoud, Hany El-Hamshary
Summary: The synthesized water-soluble polymers containing quaternary onium salts exhibited strong antimicrobial activity. Among the tested microorganisms, Aspergillus niger and Escherichia coli showed the strongest inhibition, indicating that the new compounds have low inhibition zone diameters and minimal inhibitory concentrations.
Article
Chemistry, Multidisciplinary
James C. Corcoran, Rui Guo, Yue Xia, Yi-Ming Wang
Summary: In this study, a method for the synthesis of aryl-substituted benzocycloheptenes and -hexenes using vinyl cation mediated Friedel-Crafts cyclization was reported. The hydrotriflate salt of an electron-poor pyridine was used as a unique and efficient proton source in this process. The mild conditions enabled a wide range of alkynes to be used as substrates in this scalable and convenient protocol.
CHEMICAL COMMUNICATIONS
(2022)
Article
Chemistry, Multidisciplinary
Zhonghua Li, Ruiling Ouyang, Yuechao Cao, Dandan Han, Songgu Wu, Junbo Gong
Summary: This study explores the solid-state form modification of Belinostat (PXD101) through co-crystallization with other substances to improve its water solubility and enhance the efficacy of oral formulations. The results show that the obtained multicomponent crystals have higher apparent solubility compared to PXD101 alone, with PXD101-INA cocrystal demonstrating significant inhibition of cancer cell proliferation even at low concentrations. These findings shed light on the potential of multicomponent crystals in the development of pharmaceutical products.
CRYSTAL GROWTH & DESIGN
(2022)
Article
Electrochemistry
Atsushi Kitada, Kio Kawata, Masahiro Shimizu, Masayuki Saimura, Takashi Nagata, Masato Katahira, Kazuhiro Fukami, Kuniaki Murase
Summary: This study reports a glyme-based electrolyte where ligand exchange conduction takes place. The experimental results indicate that the glyme chain length may need to be long enough to bridge Li+ ions, allowing the momentum exchange of Li+ ions via solvent molecules.
JOURNAL OF THE ELECTROCHEMICAL SOCIETY
(2021)
Review
Biochemistry & Molecular Biology
Sara Fahs, Yogita Patil-Sen, Timothy J. Snape
Review
Chemistry, Medicinal
Chris Sherer, Timothy J. Snape
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2015)
Article
Chemistry, Organic
Theodore J. Hester, Sarah R. Dennison, Matthew J. Baker, Timothy J. Snape
ORGANIC & BIOMOLECULAR CHEMISTRY
(2015)
Article
Chemistry, Organic
Dana Ameen, Timothy J. Snape
TETRAHEDRON LETTERS
(2015)
Review
Clinical Neurology
Timothy J. Snape, Tracy Warr
SEMINARS IN PEDIATRIC NEUROLOGY
(2015)
Article
Biochemistry & Molecular Biology
Yogita Patil-Sen, Sarah R. Dennison, Timothy J. Snape
BIOORGANIC & MEDICINAL CHEMISTRY
(2016)
Review
Biochemistry & Molecular Biology
Frederick Harris, Saurabh Prabhu, Sarah R. Dennison, Timothy J. Snape, Robert Lea, Manuela Mura, David A. Phoenix
PROTEIN AND PEPTIDE LETTERS
(2016)
Article
Biochemistry & Molecular Biology
Saurabh Prabhu, Sarah R. Dennison, Manuela Mura, Robert W. Lea, Timothy J. Snape, Frederick Harris
JOURNAL OF PEPTIDE SCIENCE
(2014)
Article
Medicine, Research & Experimental
Samridhi Lal, Timothy J. Snape
MEDICAL HYPOTHESES
(2014)
Review
Chemistry, Organic
Dana Ameen, Timothy J. Snape
SYNTHESIS-STUTTGART
(2015)
Article
Chemistry, Medicinal
Christopher Lawson, Thowaiba Babikr Ahmed Alta, Georgia Moschou, Vasiliki Skamnaki, Theodora G. A. Solovou, Caroline Topham, Joseph Hayes, Timothy J. Snape
Summary: Medulloblastoma is a highly aggressive and heterogeneous tumor that accounts for 15-20% of childhood brain tumors. In this study, potent in vitro anticancer activity against medulloblastoma cell lines was achieved using first-generation compounds, leading to the development of second-generation compounds with up to sixty times the activity, providing promising new leads for further research.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Bethanie Dean, Gemma Cooper, Maitreyi Shivkumar, Timothy J. Snape
Summary: A series of synthetic hydroxy-xanthones related to compounds found in Swertia plants were prepared and evaluated for their antiviral activity against human coronavirus OC43. The initial screening results in BHK-21 cell lines showed promising biological activity with a significant reduction in viral infectivity (p <= 0.05). Functionalization around the xanthone core increased the biological activity of the compounds compared to xanthone itself. Further studies are needed to determine the mechanism of action, but favorable property predictions make them attractive lead compounds for potential coronavirus treatments.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Chemistry, Medicinal
Andrea Cuppoloni, Joao Vitor Silva, Timothy James Snape, Samridhi Lal, Jeanine Giarolla
Summary: This study explored the inhibitory activity and structural-activity relationship (SAR) of a series of 2,3-arylindoles derivatives on the COX-2 enzyme using molecular docking simulations. The results showed that Gly 526 and Phe 381 residues are relevant for improving inhibitory activity on para-substituted 3-phenyl- compounds. Arg 120 residue was also demonstrated to be important for COX-2 inhibition. These structural features can be used in further drug design studies.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2023)
Review
Pharmacology & Pharmacy
Samridhi Lal, Timothy J. Snape
DRUG DISCOVERY TODAY
(2020)
Article
Biochemistry & Molecular Biology
Chris Sherer, Saurabh Prabhu, David Adams, Joseph Hayes, Farzana Rowther, Ibrahim Tolaymat, Tracy Warr, Timothy J. Snape
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
