Article
Biochemistry & Molecular Biology
Danielle O. Maia, Valdenice F. Santos, Cristina R. S. Barbosa, Yuri N. Froes, Debora F. Muniz, Ana L. E. Santos, Maria H. C. Santos, Romerio R. S. Silva, Claudio G. L. Silva, Racquel O. S. Souza, Joicy C. S. Sousa, Henrique D. M. Coutinho, Claudener S. Teixeira
Summary: The schiff base complex [Ni(L2)] showed moderate toxicity, significant leishmanicidal activity, and antibacterial effects against P. aeruginosa, but did not have clinically relevant minimum inhibitory concentration against S. aureus and E. coli. The combination of [Ni(L2)] complex with antibacterial drugs enhanced the antibiotic activity against multi-resistant strains, suggesting its potential as a promising molecule for new therapies against resistant bacteria and leishmaniasis.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Biochemistry & Molecular Biology
Alireza Foroughnia, Aliakbar Dehno Khalaji, Eskandar Kolvari, Nadiya Koukabi
Summary: A new chitosan Schiff base and its nanocomposite were synthesized and characterized, showing excellent efficiency in methyl orange removal and antibacterial activities. The presence of iron oxide nanoparticles in the nanocomposite may have contributed to its unique properties.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Biochemistry & Molecular Biology
Pruthviraj Limbachiya, Vipul Patel, Gaurang Rami, Jabali Vora
Summary: This study investigates the synthesis and characterization of two chitosan dibenzylideneacetone Schiff bases, using various analytical techniques. The antimicrobial activity of the chitosan derivatives was tested against bacterial and fungal strains, while cytotoxicity tests were conducted on different cell lines. The results demonstrate that CHDBA shows promise as a potential treatment option for breast cancer and lung cancer, as it exhibits significant effectiveness and low cytotoxicity.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Chemistry, Applied
Chuan-Hua Li, Meng-Han Ji, Kai-Wen Zhang, Shou-Ying Sun, Jian-Hong Jiang
Summary: A new bismuth(III) Schiff-base complex has been synthesized and structurally characterized. The complex exhibits high activity against bacteria and tumor cells.
APPLIED ORGANOMETALLIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Mohammed Khaled Bin Break, Tan Yew Fung, May Zie Koh, Wan Yong Ho, Mohamed Ibrahim Mohamed Tahir, Omar Ashraf Elfar, Rahamat Unissa Syed, Weam M. A. Khojali, Turki Mubarak Alluhaibi, Bader Huwaimel, Christophe Wiart, Teng-Jin Khoo
Summary: A series of novel macroacyclic Schiff base ligands and their Cu (II) complexes were synthesized and evaluated for their anticancer and antibacterial activities. Among them, Cu1 showed the highest cytotoxic activity against breast cancer cells, while compound 3 exhibited the most potent antibacterial activity against K. rhizophila and S. aureus. The results suggested that these compounds have potential applications as anticancer and antibacterial agents.
Article
Polymer Science
Zohreh Mohammadhashemi, Mohammad Jalal Zohuriaan-Mehr, Reza Jahanmardi
Summary: This study reports a facile and nearly quantitative synthesis of a novel partially bio-based Schiff base modifier for surface modification of commercial superabsorbent polymer (SAP) hydrogels. The modified SAP showed improved saline absorbency and antibacterial activity, making it a potential candidate for biomedical applications.
Article
Nanoscience & Nanotechnology
Kuiyuan Wang, Kai Chen, Timothy J. Prior, Xing Feng, Carl Redshaw
Summary: The study synthesized new double-layer Schiff base macrocycles using aldehydes, and found that one compound immobilized Pd with excellent peroxidase-like catalytic activity, exhibited outstanding bactericidal activity against Escherichia coli and Staphylococcus aureus, and showed biosafety in cytotoxicity measurements. These findings have potential to guide innovation in Pd-based composites as enzyme mimetics and antibacterial materials.
ACS APPLIED MATERIALS & INTERFACES
(2022)
Article
Chemistry, Physical
Hadi Kargar, Amir Adabi Ardakani, Muhammad Nawaz Tahir, Muhammad Ashfaq, Khurram Shahzad Munawar
Summary: In this study, a series of mononuclear Ni(II), Cu(II), and Zn(II) complexes with ONNO donor salentype Schiff base ligands were prepared and characterized. The antibacterial activities of the synthesized compounds were tested, with metal chelates showing slightly better effectiveness than free ligands.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Physical
Hadi Kargar, Amir Adabi Ardakani, Muhammad Nawaz Tahir, Muhammad Ashfaq, Khurram Shahzad Munawar
Summary: Three new mononuclear metal complexes with Salen-type tetradentate Schiff base ligand have been synthesized and characterized, showing significant antibacterial activities against various bacterial strains. Nickel and copper complexes have monoclinic crystal system, while zinc complex has orthorhombic crystal system, all with specific coordination geometries.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Multidisciplinary
Halit Muglu, Belma Zengin Kurt, Fatih Sonmez, Emre Guzel, M. Serdar Cavul, Hasan Yakan
Summary: A series of novel bis(thio/carbohydrazone) compounds were synthesized and their structures were elucidated using various spectroscopic techniques. The compounds exhibited antioxidant activity, with thiourea-based compounds showing better activity than urea-based compounds. Among them, compound 11 showed the highest antioxidant activity. DFT calculations were performed to analyze the electronic characteristics and bond properties of the compounds.
JOURNAL OF PHYSICS AND CHEMISTRY OF SOLIDS
(2022)
Article
Materials Science, Paper & Wood
Bingxin Zhao, Mingxue Yuan, Lianzhu Wang, Zhemin Liu, Xiaodan Fu, Hina Mukhtar, Changliang Zhu, Han Sun, Min Yao, Haijin Mou
Summary: Bacterial cellulose (BC) with L-arginine Schiff base was prepared and tested for its antibacterial activity. The cellulose composites showed excellent antibacterial potential against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa, making them promising candidates for biomedical applications.
Article
Chemistry, Inorganic & Nuclear
Adi Darmawan, Hasan Muhtar, Harizatuz Zakiyyah, Damar Nurwahyu Bima
Summary: New water-soluble Schiff base complexes with potential antimicrobial applications were successfully synthesized by modifying the ligand's solubility in water through the addition of a sulfonate group. The complexes showed greater solubility in water and increased antibacterial activity compared to the ligands without the sulfonate group. Meanwhile, theoretical calculations confirmed the improved solubility and reactivity of the complex with the sulfonate group, supporting its potential for antimicrobial applications.
Article
Biochemistry & Molecular Biology
Riccardo Fontana, Peggy Carla Raffaella Marconi, Antonella Caputo, Vasak B. Gavalyan
Summary: This study focused on the antimicrobial activity of novel chitosan Schiff bases (CSSB) and found that their increased solubility greatly enhanced the inhibitory effects on both Gram-positive and Gram-negative bacteria as well as yeast, opening up new possibilities for antimicrobial prevention in fields such as food, cosmetics, and restoration.
Article
Engineering, Biomedical
Dawei Li, Guoke Tang, Hui Yao, Yuqi Zhu, Changgui Shi, Qiang Fu, Fei Yang, Xing Wang
Summary: In response to the global crisis of antibiotic resistance, a new drug delivery system has been developed, which exhibits pH-responsive and programmable drug release behavior, leading to outstanding antibacterial therapy both in vitro and in vivo. The results of this study provide important guidance for the rational design of multifunctional antimicrobial vehicles.
BIOACTIVE MATERIALS
(2022)
Article
Biochemistry & Molecular Biology
Yangming Dong, Moucui Li, Yun Hao, Yunrui Feng, Yinghui Ren, Haixia Ma
Summary: In this study, fourteen novel Schiff base compounds (AS-1 to AS-14) containing 5-amino-1H-1,2,4-triazole-3-carboxylic acid and substituted benzaldehyde were synthesized and their structures were verified. The antifungal activities of the compounds against Wheat gibberellic, Maize rough dwarf and Glomerella cingulate were investigated. It was found that some compounds showed better antifungal activity than the standard drug fluconazole, and the introduction of halogen elements and electron withdrawing groups on the benzene ring improved the activity.
CHEMISTRY & BIODIVERSITY
(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)