Review
Infectious Diseases
Elham Zarenezhad, Hussein T. Abdulabbas, Mahrokh Marzi, Esraa Ghazy, Mohammad Ekrahi, Babak Pezeshki, Abdolmajid Ghasemian, Amira A. Moawad
Summary: Methicillin-resistant Staphylococcus aureus (MRSA) has developed extensive antibiotic resistance and contains virulence factors for severe infections. Nickel nanoparticles (NiNPs) have shown potential as a cheap prognostic and therapeutic agent, exerting antibacterial effects through disrupting cell membranes, deforming proteins, and inhibiting DNA replication.
Review
Chemistry, Medicinal
Dan Jiang, Bi Liu, Tao Gao
Summary: Oxazolidinone derivatives are a potential new class of antimicrobial agents with activity against multidrug-resistant Gram-positive pathogens, but are associated with significant adverse events and emerging resistance. Hybridization of oxazolidinones with other antibacterial pharmacophores can interact with multiple targets or counterbalance known side effects.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2021)
Article
Microbiology
Mohamad Hamad, Farah Al-Marzooq, Vunnam Srinivasulu, Hany A. Omar, Ashna Sulaiman, Dana M. Zaher, Gorka Orive, Taleb H. Al-Tel
Summary: We report the discovery of a new class of potent antimicrobial compounds effective against Gram-positive bacteria, including MRSA. These compounds exhibit low minimum inhibitory concentrations and rapid killing ability, without inducing bacterial resistance. Furthermore, they show minimal toxicity to human red blood cells. The study suggests that these small molecules hold promise as new antibacterial agents against MRSA infections.
FRONTIERS IN MICROBIOLOGY
(2022)
Article
Chemistry, Multidisciplinary
William B. Wang, Jude C. Clapper
Summary: This study investigates the antibacterial properties of polyacrylonitrile-based nanofibers coated with different concentrations of copper nanoparticles. The research found that these nanofibers demonstrated antibacterial activity against resistant bacteria. These nanofibers have the potential to be used on contact surfaces that are at risk of contracting bacterial infections.
Article
Chemistry, Medicinal
Dingyi Shen, Songpo Duan, Yuhan Hu, Jintong Liang, Youzhi Tang
Summary: This study found that the phloroglucinol derivative TPG and 2-nitrophloroglucinol exhibited potent synergistic antibacterial activity with penicillin or bacitracin against MRSA. The combination disrupted the MRSA cell membrane and inhibited the expression of related proteins, effectively inhibiting MRSA growth.
PHYTOTHERAPY RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Zhen Zhang, Zhujun Luo, Ying Sun, Duanyu Deng, Kaize Su, Jinxuan Li, Zhenping Yan, Xu Wang, Jifan Cao, Wende Zheng, Song Ang, Yanxian Feng, Kun Zhang, Hang Ma, Panpan Wu
Summary: This study designed and synthesized a series of novel CBD derivatives, among which derivative 21f showed enhanced antibacterial activity against MRSA without cytotoxic effect. Mechanistic studies further revealed that 21f inhibited biofilm formation, induced reactive oxygen species, and reduced bacterial metabolism, leading to accelerated bacterial death.
BIOORGANIC CHEMISTRY
(2023)
Article
Engineering, Environmental
Nuttaporn Chokesawatanakit, Pasakorn Jutakridsada, Sophon Boonlue, Jesper T. N. Knijnenburg, Phillip C. Wright, Mika Sillanpaa, Khanita Kamwilaisak
Summary: Hydrothermal reaction and photodeposition were used to transform TiO2 nanoparticles to TiO2 nanotubes loaded with Ag, showing increased surface area and antibacterial activity. Ag/TNTs exhibited antibacterial activity under UV light and could also reduce bacteria growth in the dark.
JOURNAL OF ENVIRONMENTAL CHEMICAL ENGINEERING
(2021)
Article
Immunology
Yifei Lu, Yingran Wang, Jing Wang, Yan Zhao, Qiu Zhong, Gang Li, Zhifeng Fu, Shuguang Lu
Summary: Endolysin LysP108 demonstrates promising antibacterial potential as it can lyse bacterial cell walls, inhibit bacterial biofilms, and work synergistically with vancomycin to reduce abscess size in MRSA-infected mice. The results indicate strong bactericidal effects against MRSA and the ability to significantly reduce subcutaneous abscess size when used in combination with vancomycin.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2021)
Article
Chemistry, Medicinal
Onanong Vorasin, Khanchyd Momphanao, Praewpan Katrun, Chutima Kuhakarn, Chutima Jiarpinitnun
Summary: The study identified a range of potential antibacterial vinyl sulfone derivatives, with nitrile-substituted vinyl phenyl sulfones showing the strongest activity and potentially functioning through sulfhydryl conjugation. Additionally, these compounds could also affect host cell adhesion, suggesting promising therapeutic potential for S. aureus and MRSA.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Biochemistry & Molecular Biology
In-Geun Jung, Jae-Young Jeong, Seung-Hoon Yum, You-Jin Hwang
Summary: This study screened 16 medicinal plants and found that some extracts and fractions showed significant inhibitory effects on Staphylococcus aureus, including multidrug-resistant strains, with low cytotoxicity to human cells.
Review
Chemistry, Physical
Wendy Wai Yeng Yeo, Sathiya Maran, Amanda Shen-Yee Kong, Wan-Hee Cheng, Swee-Hua Erin Lim, Jiun-Yan Loh, Kok-Song Lai
Summary: This review summarizes the current insights of using Metal-Containing NPs in treating MRSA and provides an in-depth appraisal of the opportunities and challenges in utilizing metal-NPs to treat MRSA.
Article
Chemistry, Analytical
Geunyoung Nam, Muhwan Kim, Yeonsook Jang, Sungbo Cho
Summary: A cold atmospheric pressure microplasma pipette (CAPMP) has been developed for targeted disinfection, demonstrating effective antibacterial ability that depends on treatment time and the number of layers of covering material.
Article
Acoustics
Qin Shu, Hanghang Lou, Tianyu Wei, Xinglin Zhang, Qihe Chen
Summary: The synergistic treatment of ultrasound and MEL-A showed remarkable antibacterial effect against MRSA, as evidenced by enumeration of viable microbes.
ULTRASONICS SONOCHEMISTRY
(2021)
Article
Immunology
Abderrahmen Merghni, Mohamed Ali Lassoued, Bakoliarisoa Nivomalala Voahangy Rasoanirina, Sarra Moumni, Maha Mastouri
Summary: This study analyzed the chemical composition of turpentine essential oil and developed a nanoemulsion with enhanced antibacterial and antibiofilm potential against MRSA. The nanoemulsion showed promising biofilm disruption activity.
MICROBIAL PATHOGENESIS
(2022)
Article
Pharmacology & Pharmacy
Roberto Oliva, Giovanna Ginestra, Anna Piperno, Antonino Mazzaglia, Antonia Nostro, Angela Scala
Summary: This study developed a novel PLA-PEG NPs for the delivery of Linezolid against MRSA. The encapsulation efficiency of LNZ in PLA-PEG NPs was 15% with a 10:3 polymer to drug mass ratio, and sustained release kinetics with 65% of the antibiotic released within 80 h. The NPs exhibited antimicrobial activity against various Gram-positive bacteria including MRSA, and showed inhibitory activity on both planktonic growth and preformed biofilm of MRSA.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
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)
