Review
Infectious Diseases
Ammar A. Al-Fadhli, MichaelD. Threadgill, Faez Mohammed, Paul Sibley, Wadie Al-Ariqi, Ifat Parveen
Summary: Macrolides produced by rare actinomycetes exhibit diverse biological activities, including antibacterial, antifungal, antimicrobial, antiprotozoal, and antimalarial properties. Several groups of macrolides, such as ammocidins, bafilomycins, and spinosyns, show a wide range of bioactivities. These compounds have the potential for future applications in medicine.
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS
(2022)
Article
Infectious Diseases
Ze-Hua Cui, Hui-Ling He, Zi-Jian Zheng, Zhao-Qi Yuan, Ying Chen, Xin-Yi Huang, Hao Ren, Yu-Feng Zhou, Dong-Hao Zhao, Liang-Xing Fang, Yang Yu, Ya-Hong Liu, Xiao-Ping Liao, Jian Sun
Summary: Phentolamine enhances the antibacterial activity of macrolide antibiotics against Gram-negative bacteria by reducing efflux pump activity and causing direct damage to the outer membrane leaflet.
Article
Chemistry, Organic
Gesa Hertrampf, Sandra Vojnovic, Jonas I. Mueller, Christian Merten, Jasmina Nikodinovic-Runic, Tobias A. M. Gulder
Summary: Myxocoumarin A from Stigmatella aurantiaca MYX-030 exhibits strong antifungal activity against agriculturally relevant pathogens. The total synthesis revealed its stereochemical configuration and demonstrated potent antibacterial activities against certain bacteria.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Review
Chemistry, Multidisciplinary
Kai Wei, Xinhua Zheng, Hongbin Zhang
Summary: Dioxinone derivatives have attracted attention due to their high reactivity, unique chemical properties, and potential synthetic applications. The conversion of dioxinones to acylketenes and their subsequent nucleophilic capture is an important strategy for synthesizing beta-keto acid derivatives. This review discusses recent advances in the application of dioxinones in total synthesis and synthetic method research.
FRONTIERS IN CHEMISTRY
(2022)
Article
Chemistry, Organic
Srijana Subba, Sumit Saha, Susanta Mandal, Amlan Jyoti Ghosh, Tilak Saha
Summary: The first total synthesis of aspergillolide has been achieved using commercially available compounds as the chiral resources and utilizing epoxide ring opening reaction and ring closing metathesis (RCM). In addition, a preliminary antimicrobial assay of the synthesized compound has been conducted.
TETRAHEDRON LETTERS
(2022)
Article
Plant Sciences
Michael S. Cowled, Hang Li, Cameron L. M. Gilchrist, Ernest Lacey, Yit-Heng Chooi, Andrew M. Piggott
Summary: In this study, seven new berkeleylactone analogues and six known analogues were identified from large-scale cultivation of Penicillium turbatum NRRL 5630 on rice. The structures of the berkeleylactones were determined through spectroscopic analysis and molecular modeling. Additionally, the genome of P. turbatum was sequenced, and a potential gene cluster responsible for berkeleylactone biosynthesis was identified. The new berkeleylactone analogues showed no significant biological activity, suggesting a previously undiscovered biological role.
JOURNAL OF NATURAL PRODUCTS
(2023)
Article
Immunology
Jorge Val-Calvo, Jane Darcy, James Gibbons, Alan Creighton, Claire Egan, Thomas Buckley, Achim Schmalenberger, Ursula Fogarty, Mariela Scortti, Jose A. Vazquez-Boland
Summary: This study reports the detection of a multidrug-resistant clone MDR-RE 2287 outside the United States, highlighting the risk of international spread through horse movements.
EMERGING INFECTIOUS DISEASES
(2022)
Article
Chemistry, Organic
Da Seul Lee, Saki Maejima, Michael J. Krische
Summary: The C28-C41 side-chain of neaumycin B, including a contiguous stereohextet, is synthesized in 8 steps through the longest linear sequence. Convergence is achieved by using Williams' Felkin-Anh-selective triorganozincate-mediated vinylation of an alpha,beta-stereogenic aldehyde. The relative stereochemical assignment of the C33-C35 stereotriad is determined by C-13 NMR analysis of the related acetonide, while the relative stereochemistry of C33 carbinol and C36-C37 glycidol is determined by comparative NOE analysis of the related diastereomeric furans.
Article
Chemistry, Organic
Manuel G. Schriefer, Hedda Schrey, Haoxuan Zeng, Marc Stadler, Rainer Schobert
Summary: The synthetic berkeleylactone A was shown to inhibit the formation of Staphylococcus aureus biofilms and exhibit significant dispersive effects on preformed biofilms of Candida albicans.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2021)
Review
Chemistry, Multidisciplinary
Tegan P. Stockdale, Nelson Y. S. Lam, Matthew J. Anketell, Ian Paterson
Summary: The diverse and complex structures of polyketide natural products have inspired synthetic chemists for decades. This review summarizes a thirty-year journey into the total synthesis of 18 polyketide natural products, highlighting the unique challenges and discoveries encountered along the way, with a focus on the crucial role of highly selective aldol reactions in configuring the densely oxygenated stereoclusters.
BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN
(2021)
Article
Chemistry, Organic
Hiroya Takeshita, Tomoya Sugai, Haruhiko Fuwa
Summary: A stereocontrolled synthetic approach to the C3-C17 acyclic domain of neaumycin B has been developed, involving tandem reactions, regioselective reductive opening, stereoselective formation of olefin, and asymmetric reduction for creating the stereogenic center.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Xie-Peng Liu, Wei Lv, Fei Zhao, Jing Ding, Jue-Ru Zhang, Feng Xue, Jian-Zhong Zhang, Li-Yong Liu, Mark Cushman, Yun Li, Jian-Hua Liang
Summary: The hybrids of macrolides and quinolones bridged with linkers from 11,12-cyclic carbamate of macrolides showed different structure-activity relationships and improved metabolic stability compared to telithromycin. The optimized macrolone was 38-fold more potent than telithromycin against A2058/2059-mutated Mycoplasma pneumoniae, potentially due to a novel mode of action between the carboxylic acid of quinolone moiety and the bacterial ribosome.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Review
Polymer Science
Md. Amdadul Huq, Md. Ashrafudoulla, M. Mizanur Rahman, Sri Renukadevi Balusamy, Shahina Akter
Summary: Green synthesis of silver nanoparticles using biological resources is a convenient, economical, and environmentally friendly method. Plant extracts and microorganisms can act as reducing and capping agents in the synthesis of silver nanoparticles. These biosynthesized silver nanoparticles have potential applications in biomedical science, particularly as antibacterial agents.
Review
Chemistry, Organic
Debobrata Paul, Subhendu Das, Sanu Saha, Himangshu Sharma, Rajib Kumar Goswami
Summary: The intramolecular Heck reaction plays a significant role in synthesizing natural products by constructing various cyclic scaffolds. It serves as a strategic step in the synthesis of different natural products.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Agriculture, Multidisciplinary
Hongde Li, Shang Wu, Xiong Yang, Hongfu He, Zengxue Wu, Baoan Song, Runjiang Song
Summary: The study revealed a series of novel indole derivatives with antibacterial activity and identified a new compound with higher activity, which could potentially be utilized in the modern pesticide industry.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2022)
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)