Article
Agriculture, Multidisciplinary
Yu-Bin Bai, Meng Zhang, Ding Li, Yu Zhao, Liang-Zhu Huang, Jin-Ming Gao
Summary: Researchers synthesized 39 diversified griseofulvin derivatives and found that compounds 5h and 5l exhibited excellent antifungal activity against two phytopathogenic fungi. Compounds 9, 10, 11, and 12 also showed potential antifungal activity.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Jian-Chuan Liu, Jian Yang, Shu-Xin Lei, Ming-Fan Wang, Yan-Ni Ma, Rui Yang
Summary: In this study, a series of new biphenyl compounds based on natural biphenyl phytoalexins were designed, synthesized, and evaluated for their antifungal activities against four invasive fungi. Promising compounds with remarkable antifungal activity were discovered through modifying the two benzene rings of a well-known biphenyl phytoantitoxin. Notably, compounds 23a, 23e, and 23h exhibited potent activities and a broad antifungal spectrum, with low minimum inhibitory concentrations (MICs) and comparable potency to the positive control amphotericin B against Cryptococcus neoformans. Preliminary mechanism studies suggested that compound 23h exerts its rapid fungicidal activity by disrupting the fungal cell membrane. Moreover, compound 23h displayed significant inhibition against virulence factors of Cryptococcus neoformans, low toxicity to normal human cells, and favorable pharmacokinetic and drug-like properties. These results highlight the bright and promising strategy of developing new antifungal candidates derived from natural phytoalexins.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Applied
Hong-Lei Xu, Yan Wei, Shuanghong Hao
Summary: A series of thioether derivatives containing 4-methylumbelliferone fused oxazole moiety were designed and synthesized, and their antifungal activity, as well as their protective and curative effects against B. cinerea on tomato fruits, were evaluated. The environmental toxicity of these compounds against A. salina was also assessed.
NATURAL PRODUCT RESEARCH
(2022)
Article
Agriculture, Multidisciplinary
Hu Li, Ying-Hui He, Yong-Mei Hu, Qing-Ru Chu, Yong-Jia Chen, Zhen-Rong Wu, Zhi-Jun Zhang, Ying-Qian Liu, Cheng-Jie Yang, Hong-Jie Liang, Yin-Fang Yan
Summary: This study synthesized and tested 30 magnolol derivatives based on natural products, with 11 compounds showing potential antifungal activity against four plant pathogenic fungi. Compound L5 exhibited strong antifungal properties against Botrytis cinerea, suggesting it as a promising candidate for crop protection.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2021)
Article
Agriculture, Multidisciplinary
Xiang Cheng, Zonghan Xu, Huisheng Luo, Xihao Chang, Xianhai Lv
Summary: A series of pyrazol-5-yl-benzamide derivatives containing the oxazole group were synthesized as potential SDH inhibitors. Most of these compounds displayed moderate-to-excellent in vitro antifungal activities against various fungi. Compounds C13 and C14 exhibited significant inhibitory activities against S. sclerotiorum and showed protective effects on crop leaves.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Yucong Ma, Lu Wang, Aidang Lu, Wei Xue
Summary: A series of oxazinyl flavonoids were synthesized based on flavone and their activities against tobacco mosaic virus (TMV) and plant pathogenic fungi were investigated. The compounds exhibited moderate to excellent antiviral activities against TMV, with some even surpassing commercially available antiviral agents. They also displayed broad-spectrum fungicidal activities against six kinds of plant pathogenic fungi.
Article
Biochemistry & Molecular Biology
Wataru Miyanishi, Makoto Ojika, Dai Akase, Misako Aida, Yasuhiro Igarashi, Yukishige Ito, Yu Nakagawa
Summary: The study found that attachment of 2-aminoethanol to the carboxy group of PRM-A significantly suppressed aggregation, and the prepared amide derivatives not only bound to Man without aggregation but also exhibited antifungal activity.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Organic
Christian P. Bold, Cindy Klaus, Bernhard Pfeiffer, Jasmine Schurmann, Rafael Lombardi, Daniel Lucena-Agell, J. Fernando Diaz, Karl-Heinz Altmann
Summary: The synthesis of an oxazole-based analog of (-)-zampanolide was studied, with successful construction of (-)-dactylolide analog 22. However, attempts to attach (Z,E)-sorbamide failed, possibly due to the migration of the C(8)-C(9) double bond in the macrocycle. This limitation may affect the utility of zampanolide analogs with aromatic moieties as tetrahydropyran replacements.
Article
Chemistry, Multidisciplinary
Alexander O. Brachmann, Silke I. Probst, Joel Ruethi, Darya Dudko, Helge B. Bode, Joern Piel
Summary: This study identified a cryptic biosynthetic locus encoding an N-acyltransferase and a non-heme diiron desaturase-like enzyme in a bacterium producing labradorin through transposon mutagenesis. Heterologous expression in E. coli demonstrated the ability of both enzymes to produce indolyloxazoles, and stable-isotope feeding experiments provided evidence for an unusual desaturase mechanism generating the oxazole by decarboxylative cyclization.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Chemistry, Organic
Yu Nakagawa, Yuzuka Oya, Makoto Ojika, Yasuhiro Igarashi, Yukishige Ito
Summary: This study discovered that the modified derivatives of C4'-N-formyl PRM-A and C4'-N-acetyl PRM-A showed significant antifungal activities without forming aggregates or precipitates, providing a new strategy for the therapeutic application of PRM-A.
Article
Chemistry, Multidisciplinary
Zhiqiang Ren, Zhongliu Sun, Yifei Li, Xin Fan, Mingda Dai, Yunxia Wang, Xiangdong Hu
Summary: A new synthetic strategy was reported for the first-time asymmetric synthesis of three compounds belonging to the Cephalotaxus diterpenoids class, featuring a diastereoselective Pauson-Khand reaction and a ring-closing metathesis/elimination protocol for the core tetracyclic skeleton and tropone moiety construction.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Review
Biochemistry & Molecular Biology
Evan P. Vanable, Laurel G. Habgood, James D. Patrone
Summary: Natural products, with their complex structures, diversity, and biological activity, have inspired chemists and driven technological advancements. The field of natural product synthesis continuously evolves, improving selectivity, yield, scalability, and more. One interesting and unique technique is the use of chemoenzymatic reactions in the synthesis of natural products.
Correction
Biochemistry & Molecular Biology
Christopher J. Huck, Yaroslav D. Boyko, David Sarlah
Summary: The article is a correction regarding dearomative logic in natural product total synthesis by Christopher J. Huck et al. The authors present a new method that can be applied effectively in the synthesis of natural products and provide relevant examples.
NATURAL PRODUCT REPORTS
(2022)
Article
Chemistry, Multidisciplinary
Yoshio Ando, Takumi Fukazawa, Ken Ohmori, Keisuke Suzuki
Summary: This study describes the synthesis of a monomer, hemi-actinorhodin, as a model target in the synthetic study of dimeric pyranonaphthoquinone antibiotics. Several implications were gained, including stereoselective synthesis of the pyranonaphthoquinone, viable construction of the naphthazarin core, and final deprotection conditions.
BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN
(2021)
Article
Infectious Diseases
Chi-Jan Lin, Ya-Lin Chang, Yu-Liang Yang, Ying-Lien Chen
Summary: The study demonstrates that tryptanthrin possesses novel antifungal activity against Cryptococcus species by interfering with the cell cycle and signaling pathways, indicating its potential as a drug or adjuvant for the treatment of cryptococcosis.
Article
Polymer Science
Zhonghe Sun, Mu Wang, Zhi Li, Bonnie Choi, Roger J. Mulder, Anchao Feng, Graeme Moad, San H. Thang
Article
Chemistry, Analytical
Biagia Musio, Rosa Ragone, Stefano Todisco, Antonino Rizzuti, Mario Latronico, Piero Mastrorilli, Stefania Pontrelli, Nicola Intini, Pasquale Scapicchio, Maurizio Triggiani, Tommaso Di Noia, Domenico Acquotti, Cristina Airoldi, Michael Assfalg, Alessandro Barge, Lorraine Bateman, Francesca Benevelli, Davide Bertelli, Fabio Bertocchi, Aurimas Bieliauskas, Anna Borioni, Augusta Caligiani, Emanuela Callone, Ales Camra, Flaminia Cesare Marincola, Dinesh Chalasani, Roberto Consonni, Paolo Dambruoso, Silvia Davalli, Taylor David, Bernd Diehl, James Donarski, Ana M. Gil, Roberto Gobetto, Luca Goldoni, Erwann Hamon, John S. Harwood, Andrea Kobrlova, Francesco Longobardi, Renzo Luisi, Domenico Mallamace, Stefano Mammi, Magali Martin-Biran, Pierluigi Mazzei, Andrea Meie, Salvatore Milone, Dolores Molero Vilchez, Roger J. Mulder, Claudia Napoli, Daniele Ragno, Antonio Randazzo, Maria Cecilia Rossi, Archimede Rotondo, Algirdas Sackus, Elena Saez Barajas, Elisabetta Schievano, Bhavaraju Sitaram, Livio Stevanato, Panteleimon G. Takis, Jan Teipel, Freddy Thomas, Elisabetta Torregiani, Daniela Valensin, Marina Veronesi, John Warren, Julien Wist, Elina Zailer-Hafer, Cristiano Zuccaccia, Vito Gallo
Article
Chemistry, Medicinal
Doralyn S. Dalisay, Evan W. Rogers, Tadeusz E. Molinski
Summary: Oceanapiside (OPS) is a marine natural product that exhibits fungicidal activity against fluconazole-resistant Candida glabrata, affecting the budding patterns of cells and disrupting actin assembly, while influencing the synthesis pathway of internal sphingolipids. OPS has a mechanism of action different from traditional antifungal drugs, inhibiting fungal sphingolipid metabolism by specifically targeting the conversion of phytosphingosine to phytoceramide.
Article
Biochemistry & Molecular Biology
Angelica Faith L. Suarez, April Dawn G. Tirador, Zenith M. Villorente, Cathrina F. Bagarinao, Jan Vincent N. Sollesta, Gerard G. Dumancas, Zhe Sun, Zhao Qi Zhan, Jonel P. Saludes, Doralyn S. Dalisay
Summary: This study investigated the antibacterial and antioxidant activities of honey from Apis mellifera and Tetragonula biroi in the Philippines, revealing that honey produced by T. biroi has higher flavonoid and phenolic content compared to A. mellifera, and identified the compound responsible for its antibacterial activity. These findings suggest that Philippine honey, particularly from T. biroi, may have potential antibiotic and antioxidant properties.
Article
Chemistry, Medicinal
Kim Jye Lee-Chang, Matthew C. Taylor, Guy Drummond, Roger J. Mulder, Maged Peter Mansour, Mina Brock, Peter D. Nichols
Summary: This study demonstrates the regiospecificity of the TAG fraction from Australian thraustochytrid Aurantiochytrium sp. strain TC 20, with DHA concentrated in the sn-2 position. The concentration of sn-2 DHA in thraustochytrid TC 20 oil is higher compared to tuna oil.
Article
Engineering, Chemical
Dongyun Wu, Rujing Hou, Chunhai Yi, Stefan J. D. Smith, Jiawen Fu, Derrick Ng, Cara M. Doherty, Roger J. Mulder, Zongli Xie, Matthew R. Hill
Summary: This study investigates the anti-aging properties of PAF-1 and p-DCX in a highly selective polyimide (PI) polymer for industrial CO2 separation. The PI membranes showed slower CO2 aging rates and significantly enhanced CO2 permeability with the addition of PAF-1 and p-DCX, surpassing 2008 Upper Bounds for both CO2/N2 and CO2/CH4 separation in mixed-gas performance.
SEPARATION AND PURIFICATION TECHNOLOGY
(2021)
Article
Multidisciplinary Sciences
Yingyi Huang, Mahdokht Shaibani, Tanesh D. Gamot, Mingchao Wang, Petar Jovanovic, M. C. Dilusha Cooray, Meysam Sharifzadeh Mirshekarloo, Roger J. Mulder, Nikhil Medhekar, Matthew R. Hill, Mainak Majumder
Summary: The authors present a saccharide-based binder system to regulate polysulfides migration and improve the cycle life of Li-S batteries, achieving 97% sulfur utilization with 1000 cycles of stable performance. This innovative binder also promotes the formation of a desirable microstructure, leading to a pouch cell prototype with high specific energy, demonstrating promising potential for practical applications.
NATURE COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
David E. Williams, Kalindi D. Morgan, Doralyn S. Dalisay, Teatulohi Matainaho, Elodie Perrachon, Noemie Viller, Mailys Delcroix, Jeanne Gauchot, Haruka Niikura, Brian O. Patrick, Katherine S. Ryan, Raymond J. Andersen
Summary: This study discovered two bacterial strains with biosynthetic abilities from tropical and temperate Pacific Ocean sediment habitats. These strains produced salinorcinol, salinacetamide, and a new aminoquinone polyketide through cultivation, which are putative shunt products of the widely distributed rifamycin biosynthetic pathway.
Article
Materials Science, Multidisciplinary
Stefan J. D. Smith, Colin D. Wood, Paul H. M. Feron, Hamidreza Mahdavi, Roger J. Mulder, Cara M. Doherty, Matthew R. Hill, Xavier Mulet
Summary: Combining desired material properties into a single material for gas separations in industry remains a challenge. In this study, a family of polymer liquids inspired by hyper-crosslinked polymers (HCPs) was reported, which showed good volumetric capacity, improved selectivity, and efficient regeneration. The liquids also had low heat of adsorption and specific heat capacity, indicating favorable process thermodynamics.
SCIENCE CHINA-MATERIALS
(2022)
Article
Engineering, Chemical
Yanjie Xu, Qi Yang, Graeme Puxty, Hai Yu, William Conway, Mengxiang Fang, Tao Wang, Roger J. Mulder
Summary: Reducing water content, increasing organic character of absorbent molecules, and using non-aqueous diluents to substitute water are effective ways to improve absorbent performance. This study evaluated the diffusivity of component molecules in different blends and found that water-lean blends were more sensitive to CO2 loading and water content. The introduction of N-methyl-2-pyrrolidone weakened intermolecular interactions and had a significant impact on diffusivity, especially at higher temperatures.
INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH
(2022)
Article
Construction & Building Technology
Zhao Qing Tang, Felipe Basquiroto de Souza, Roger J. Mulder, Wenhui Duan, Wenhui Duan
Summary: This study investigated the nucleation and growth mechanism of sodium aluminosilicate hydrate (NASH) gel in geopolymer concrete. The findings revealed the presence of intermediate phases, including prenucleation clusters and partially polymerized globules, before the formation of the geopolymeric network.
CEMENT AND CONCRETE RESEARCH
(2022)
Article
Chemistry, Inorganic & Nuclear
Jett T. Janetzki, Maxim G. Chegerev, Gemma K. Gransbury, Robert W. Gable, Jack K. Clegg, Roger J. Mulder, Guy N. L. Jameson, Alyona A. Starikova, Colette Boskovic
Summary: Spin crossover complexes with the ability to switch between low spin and high spin states have potential applications in sensing, displays, and molecular electronics. This study focuses on dinuclear spin crossover complexes and investigates the influence of bridging ligands on the spin crossover behavior. The synthesis and characterization of three complexes are reported, and both solid-state and solution measurements are performed to gain insights into the interconversion between different spin states.
INORGANIC CHEMISTRY
(2023)
Review
Polymer Science
Yuankai Zhao, Roger J. Mulder, Shadi Houshyar, Tu C. Le
Summary: Polymers are important materials with diverse properties, and machine learning has shown great potential in data-driven polymer design. Machine learning models trained on polymer datasets can accurately predict polymer properties and assist in candidate polymer screening before lab synthesis.
Review
Integrative & Complementary Medicine
Muhammad Faiz Zulkifli, Mohd Naim Fadhli Mohd Radzi, Jonel P. Saludes, Doralyn S. Dalisay, Wan Iryani Wan Ismail
Summary: Honey has potential therapeutic properties for obesity control and related diseases treatment. It can reduce blood sugar levels, improve insulin sensitivity, and lipid metabolism, thus reducing the risk of obesity.
JOURNAL OF EVIDENCE-BASED INTEGRATIVE MEDICINE
(2022)
Article
Pharmacology & Pharmacy
Monika Szabo, Wioleta Kowalczyk, Anna Tarasova, Jessica Andrade, Cheang Ly Be, Roger Mulder, Jacinta White, Adam G. Meyer, Kjiana E. Schwab, Kellie Cartledge, Tu C. Le, Anoja Wickrama Arachchilage, Xiaoli Wang, Ronald Hoffman, Susan K. Nilsson, David N. Haylock, David A. Winkler
Summary: Myelofibrosis is a life-threatening blood cancer, and current drugs only provide symptomatic relief without altering the course of the disease. Inhibition of thrombopoietin, an important cytokine for platelet production, shows promise in slowing or stopping MF progression. Computational modeling and rational residue substitutions have identified a lead cyclic peptide, 48, as essential for activity at the c-Mpl receptor. These peptides are significant tools for in vivo analysis and a step towards disease-modifying therapies for MF.
ADVANCED THERAPEUTICS
(2021)
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)
