Article
Biochemistry & Molecular Biology
Dandan Peng, Jingqun Shan, Zhiwei Fan, Caoxing Huang, Haili Chen, Xinxing Wu
Summary: The limited anti-fungal activity of enzymatic hydrolysis lignin (EHL) has been overcome by cinnamaldehyde modification, which effectively enhances its anti-fungal activity. The modified lignin (EHL-DC) showed significantly improved inhibitory concentrations against Aspergillus niger and other fungi, causing changes in fungal cell membranes and reduction in mycelial biomass. This study provides valuable insights into the high-value utilization of enzymatic hydrolysis lignin using green chemistry principles.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Materials Science, Multidisciplinary
Slimane Abdous, Mehdi Derradji, Oussama Mehelli, Raouf Belgacemi, Azzedine Khadraoui, Yacine Laichi, Hamza Djerra, Noureddine Ramdani, Wenbin Liu
Summary: In this study, three new energetic benzoxazine monomers were synthesized via a one-step Mannich reaction process with explosive nitro groups incorporated in different positions. The synthesized monomers were characterized by various techniques and their thermomechanical properties and thermal stability were evaluated. The para position was found to provide the highest calorific value and the monomer ignited at 267 degrees Celsius.
MATERIALS TODAY COMMUNICATIONS
(2021)
Article
Polymer Science
Fusun Seyma Gungor
Summary: A compound with a phenolic group was successfully synthesized and subjected to Mannich reactions with primary amine compounds and paraformaldehyde, resulting in three thermally polymerizable naphthoxazines with high yields. The structures of the exchange products were characterized using analytical techniques and the ring-opening polymerization behavior was investigated.
EUROPEAN POLYMER JOURNAL
(2023)
Article
Chemistry, Medicinal
Arunadevi Mani, Anis Ahamed, Daoud Ali, Saud Alarifi, Idhayadhulla Akbar
Summary: This study successfully synthesized dopamine-associated vanillin Mannich base derivatives using a green chemistry approach, and evaluated their antioxidant and anti-tyrosinase activities. Compound 1e and 1k showed promising results in both antioxidant and anti-tyrosinase assays, indicating their potential as effective molecules in these activities.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2021)
Article
Biochemistry & Molecular Biology
Balint Lorinczi, Peter Simon, Istvan Szatmari
Summary: This study presents a new synthesis method for triarylmethane derivatives containing two biologically potent skeletons through the Mannich reaction. It may contribute to the synthesis of new neuroprotective compounds.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Polymer Science
Abdelwahed Berrouane, Mehdi Derradji, Karim Khiari, Oussama Mehelli, Abdelmalek Habes, Slimane Abdous, Bouchra Amri, Mohamed El Amine Kadi, Wenbin Liu
Summary: A novel bio-based benzoxazine monomer, Q-Bz, was synthesized through the Mannich condensation reaction using Quercetin, paraformaldehyde, and aniline. The chemical structure was confirmed by 1H NMR and FTIR. The curing behavior and polymerization process were studied using DSC and FTIR, respectively. The resulting bio-based thermoset, PQ-Bz, showed high thermal stability and processability, making it a potential sustainable alternative to petroleum-based thermosets in high-performance applications.
HIGH PERFORMANCE POLYMERS
(2023)
Article
Polymer Science
Sarah Soudjrari, Mehdi Derradji, Bouchra Amri, Khawla Djaber, Oussama Mehelli, Sana Tazibet, Slimane Abdous, Noureddine Ramdani, Wenbin Liu, Azzedine Khadraoui
Summary: Benzoxazine containing phthalonitrile is an advanced high performance thermosetting resin that has attracted significant attention. Researchers have developed a new benzoxazine containing phthalonitrile system using the renewable natural resource vanillin, which offers a simple synthesis process and autocatalytic polymerization mechanism. The newly developed monomers exhibit excellent thermal stability and thermomechanical properties.
HIGH PERFORMANCE POLYMERS
(2022)
Article
Polymer Science
Slimane Abdous, Mehdi Derradji, Oussama Mehelli, Raouf Belgacemi, Sarah Soudjrari, Noureddine Ramdani, Karim Khiari, Mohamed El Amine Kadi, Wenbin Liu
Summary: In a study aimed at developing new synthetic routes for energetic materials, two new energetic benzoxazine monomers were synthesized using a two-step Mannich reaction process. The results showed that the benzoxazine monomer based on 2,4-dinitrophenylhydrazine exhibited superior energetic properties. This study demonstrates the potential of using the Mannich reaction to synthesize benzoxazine resins for energetic applications.
HIGH PERFORMANCE POLYMERS
(2022)
Article
Chemistry, Medicinal
Swikriti Swikriti, Ritchu Babbar, Deepika Saini, Ravi Rawat, Sridevi Chigurupati, Shatha G. Felemban, Celia Vargas-De-La-Cruz, Tapan Behl
Summary: The aim of this study was to design and synthesize a series of neoteric benzylidene amino-benzimidazole derivatives and evaluate their anti-inflammatory and antioxidant potential. The designed target scaffolds were synthesized and assessed for their in vitro antioxidant activity and in vivo anti-inflammatory potential. Results showed that compounds 6c and 6j exhibited remarkable antioxidant and anti-inflammatory effects, followed by compounds 6f, 6e, and 6i. Molecular docking studies supported the in vitro and in vivo findings.
FUTURE MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Applied
Xuan Yuan, Yijia Zhou, Yudan Wang, Lijia Liu, Guoxing Yang
Summary: A bio-based compound with excellent antibacterial activity was synthesized and used to prepare films with antibacterial and anti-ultraviolet properties, suitable for fruit preservation packaging.
CARBOHYDRATE POLYMERS
(2024)
Article
Biochemistry & Molecular Biology
Sellamuthu Anbu, Anup Paul, Kalpana Surendranath, Ahmed Sidali, Armando J. L. Pombeiro
Summary: The sensor NPP demonstrates a significant enhancement in fluorescence emission upon binding with Cu2+ and can be used for both fluorescent and colorimetric detection in an aqueous medium. It was also successfully applied as a fluorescent probe for detecting Cu2+ in live cancer cells, showing recovery of emission intensity upon complex formation and reversible response to Cu2+ and EDTA in solution.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2021)
Article
Chemistry, Applied
Slimane Abdous, Mehdi Derradji, Karim Khiari, Oussama Mehelli, Abdeljalil Zegaoui, Wenbin Liu
Summary: A new class of energetic green benzoxazine polymers was developed using vanillin as a renewable reactant. The monomers were synthesized through the reaction of vanillin with compounds containing exploshores groups, specifically 2,4-dinitrophenylhydrazine and para-nitroaniline. The resulting polymers showed promising energetic performances and high thermal stability, making them suitable as reactive structure materials.
JOURNAL OF ENERGETIC MATERIALS
(2023)
Article
Biochemistry & Molecular Biology
Songul Boy, Fikret Turkan, Murat Beytur, Abdulmelik Aras, Onur Akyildirim, Halide Sedef Karaman, Haydar Yuksek
Summary: Novel N-Mannich bases were synthesized through the Mannich reaction, followed by the synthesis of eight new compounds. These compounds exhibited inhibitory activity against AChE, BChE, and GST enzymes, with the most active inhibitors showing interactions through hydrophobic and hydrogen bonding with the enzymes.
BIOORGANIC CHEMISTRY
(2021)
Review
Pharmacology & Pharmacy
Xian-Guang Bai, Yunyun Zheng, Jinxu Qi
Summary: Thiosemicarbazone Schiff base complexes have the potential to be effective anti-lung cancer drugs, and their structural diversity offers pharmaceutical chemists a wide range of possibilities. These ligands and complexes play crucial roles in anti-lung cancer treatment, but there are still challenges to overcome.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Samra Farooq, Ihsan-Ul Haq, Naseem Ullah
Summary: A series of N-Mannich base derivatives of 2-phenyl-2-imidazoline with substituted amines were designed, synthesized, and evaluated for their biological activities. The compounds showed good antioxidant, antimicrobial, and anti-inflammatory responses, with SP11 and SP13 exhibiting notable activity. SP2 demonstrated significant inhibition against alpha-amylase enzyme.
ARABIAN JOURNAL OF CHEMISTRY
(2021)
Article
Infectious Diseases
Ghayah Bahatheg, Rajesh Kuppusamy, Muhammad Yasir, David StC Black, Mark Willcox, Naresh Kumar
Summary: This study describes the development of short cationic peptoids with activity against Staphylococcus aureus strains from keratitis. The peptoids showed good antimicrobial activity against multiple strains, making them a promising class of antimicrobials.
Review
Chemistry, Multidisciplinary
Manuela Curcio, Orazio Vittorio, Jessica Lilian Bell, Francesca Iemma, Fiore Pasquale Nicoletta, Giuseppe Cirillo
Summary: This review focuses on the unique application of self-assembling nanoparticles (SANPs) based on hyaluronic acid (HA) in cancer therapy. By combining the targeting activity of HA towards cancer cells with the advantages of self-assembling nanosystems, these SANPs can be used to fabricate delivery devices. The review analyzes the pros and cons of different nanosystems based on HA and discusses the most promising strategies for further research and therapeutic protocol development.
Article
Oncology
Tessa Gargett, Lisa M. Ebert, Nga T. H. Truong, Paris M. Kollis, Kristyna Sedivakova, Wenbo Yu, Erica C. F. Yeo, Nicole L. Wittwer, Briony L. Gliddon, Melinda N. Tea, Rebecca Ormsby, Santosh Poonnoose, Jake Nowicki, Orazio Vittorio, David S. Ziegler, Stuart M. Pitson, Michael P. Brown
Summary: Targeting the tumor-associated antigen GD2 using CAR-T-cell therapy has shown promising results in controlling tumor growth in primary glioblastoma. Highly functional GD2-specific CAR-T cells can be produced using an approved clinical manufacturing process. The use of markers identified in the study has further improved tumor control rates.
JOURNAL FOR IMMUNOTHERAPY OF CANCER
(2022)
Article
Oncology
Evangeline R. Jackson, Ryan J. Duchatel, Dilana E. Staudt, Mika L. Persson, Abdul Mannan, Sridevi Yadavilli, Sarah Parackal, Shaye Game, Wai Chin Chong, W. Samantha N. Jayasekara, Marion Le Grand, Padraic S. Kearney, Alicia M. Douglas, Izac J. Findlay, Zacary P. Germon, Holly P. McEwen, Tyrone S. Beitaki, Adjanie Patabendige, David A. Skerrett-Byrne, Brett Nixon, Nathan D. Smith, Bryan Day, Neevika Manoharan, Sumanth Nagabushan, Jordan R. Hansford, Dinisha Govender, Geoff B. McCowage, Ron Firestein, Meegan Howlett, Raelene Endersby, Nicholas G. Gottardo, Frank Alvaro, Sebastian M. Waszak, Martin R. Larsen, Yolanda Colino-Sanguino, Fatima Valdes-Mora, Andria Rakotomalala, Samuel Meignan, Eddy Pasquier, Nicolas Andre, Esther Hulleman, David D. Eisenstat, Nicholas A. Vitanza, Javad Nazarian, Carl Koschmann, Sabine Mueller, Jason E. Cain, Matthew D. Dun
Summary: Diffuse midline gliomas are highly lethal childhood cancers. Palliative radiotherapy is the only established treatment with limited survival benefits. ONC201, a combination of a DRD2 antagonist and ClpP agonist, has shown promising preclinical and emerging clinical efficacy in treating diffuse intrinsic pontine gliomas. Further research is needed to understand the mechanisms of response, the impact of recurring genomic features, and the potential combination therapy with a brain penetrant PI3K/Akt inhibitor, paxalisib.
Article
Infectious Diseases
Rajesh Kuppusamy, Muhammad Yasir, Tsz Tin Yu, Florida Voli, Orazio Vittorio, Michael J. Miller, Peter Lewis, David StC Black, Mark Willcox, Naresh Kumar
Summary: There is an urgent need for new antimicrobial agents to address the global increase in antibiotic resistance. This study focused on producing short amphiphilic antibacterial and antibiofilm agents by modifying the hydrophobic and cationic groups of anthranilamide peptidomimetics. The addition of a lysine cationic group at the tail position significantly enhanced activity against E. coli and reduced cytotoxicity against mammalian cells. These compounds demonstrated notable disruption of preformed biofilms of S. aureus at micromolar concentrations.
Article
Biochemistry & Molecular Biology
Katrina Browne, Rajesh Kuppusamy, William R. Walsh, David StC Black, Mark D. P. Willcox, Naresh Kumar, Renxun Chen
Summary: Antibiotic resistance is a global challenge, and combination therapies using antibiotics and antimicrobial peptidomimetics can mitigate the development of resistance in bacteria. This strategy demonstrates synergistic activity against both Gram-positive and Gram-negative bacteria and has significant potential in clinical applications.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Crystallography
Christopher E. Marjo, Anne M. Rich, Mohan M. Bhadbhade, Saroj Bhattacharyya, Songyan Yin, David M. Miskovic, Vina R. Aldilla, Naresh Kumar
Summary: This study investigates a layered crystal system with hydrogen-bonded chloro-s-triazine rings functionalised with alkyl or fluoroalkyl chains. The results show that the crystal undergoes a thermally-induced phase transition when substituted with N-propyl chains, but the phase transition is successfully suppressed when replaced with fluorinated N-propyl chains. The study also suggests that short-chain fluoroalkanes can exert strong control over the assembly and stability of an organic crystal.
Article
Medicine, General & Internal
Jeremy Ariey-Bonnet, Raphael Berges, Marie-Pierre Montero, Baptiste Mouysset, Patricia Piris, Kevin Muller, Guillaume Pinna, Tim W. Failes, Greg M. Arndt, Philippe Morando, Nathalie Baeza-Kallee, Carole Colin, Olivier Chinot, Diane Braguer, Xavier Morelli, Nicolas Andre, Manon Carre, Emeline Tabouret, Dominique Figarella-Branger, Marion Le Grand, Eddy Pasquier
Summary: This study identified targetable vulnerabilities in glioblastoma using high-throughput screening, target deconvolution, and functional genomics. They validated the role of the top gene hit and discovered pharmacological synergisms through drug combination screens. The efficacy of the AURKA/BET inhibitor combination in glioblastoma was confirmed in pre-clinical models.
Article
Infectious Diseases
Sahil Shandil, Tsz Tin Yu, Shekh Sabir, David StC. Black, Naresh Kumar
Summary: As bacteria develop resistance against antimicrobials, alternative methods to tackle this issue must be developed. In this study, quinazolinone inhibitors were designed using molecular docking to target the pqs system in P. aeruginosa. Compound 6b showed the highest pqs inhibitory activity and no bacterial growth inhibition.
Article
Infectious Diseases
Umme Laila Urmi, Samuel Attard, Ajay Kumar Vijay, Mark D. P. Willcox, Naresh Kumar, Salequl Islam, Rajesh Kuppusamy
Summary: The development of potent antiviral agents is crucial for combating viral infections worldwide. In this study, the antiviral potential of 17 peptidomimetic compounds was evaluated against MHV-1 and HSV-1. Compounds 11 and 14 showed the most potent inhibitory effects, and they were found to directly influence the viral envelope. These findings suggest that peptidomimetic compounds could offer a new approach for the development of potent antiviral agents.
Article
Chemistry, Multidisciplinary
Patricia Piris, Duje Buric, Toshihide Yamasaki, Paul Huchede, Mailys Rossi, Melanie Matteudi, Marie-Pierre Montero, Anne Rodallec, Romain Appay, Christine Roux, Sebastien Combes, Eddy Pasquier, Marie Castets, Nicolas Andre, Paul Bremond, Manon Carre
Summary: Brain tumors, particularly glioblastoma and medulloblastoma, are highly lethal and difficult to treat. This study presents a novel approach using alkoxyamines and a bioconjugate called ALK4-MMPp to inhibit the progression of these tumors. The compounds showed promising results in in vitro and in vivo experiments, suggesting their potential as effective anticancer drug candidates. The study also developed innovative models to monitor treatment response and demonstrated the selective targeting of tumor cells without significant damage to normal brain tissue.
Meeting Abstract
Oncology
Andria Rakotomalala, Paul Lewandowski, Quentin Bailleul, Clara Savary, Melanie Arcicasa, Christine Bal, Maud Hamadou, Paul Huchede, Audrey Restouin, Remy Castellano, Yves Collette, Audrey Vincent, Pierre-Olivier Angrand, Eric Adriaenssens, Xuefen Le Bourhis, Pierre Leblond, Marie Castets, Eddy Pasquier, Alessandro Furlan, Samuel Meignan
Meeting Abstract
Oncology
Izac Findlay, Dilana Staudt, Padraic Kearney, Holly McEwen, Ryan Duchatel, Evangeline Jackson, Tyrone Beitaki, Nathan Smith, Nicholas Vitanza, Ron Firestein, Jason Cain, Sabine Mueller, Eddy Pasquier, Carl Koschmann, Esther Hulleman, Javad Nazarian, Mitchell Hansen, Frank Alvaro, Melissa Davis, Sebastian Waszak, Matthew Dun
Meeting Abstract
Oncology
Evangeline Jackson, Ryan Duchatel, Mika Persson, Abdul Mannan, Sridevi Yadavilli, Sarah Parackal, Shaye Game, Wai Chin Chong, Samantha Jayasekara, Marion Le Grand, Padraic Kearney, Alicia Douglas, Izac Findlay, Dilana Staudt, Zacary Germon, David Skerrett-Byrne, Brett Nixon, Nathan Smith, Esther Hulleman, Bryan Day, Geoffrey McCowage, Frank Alvaro, Sebastian Waszak, Martin Larsen, Yolanda Colino-Sanguino, Fatima Valdes-Mora, Andria Rakotomalala, Samuel Meignan, Eddy Pasquier, Nicholas Vitanza, Javad Nazarian, Carl Koschmann, Jason Cain, Sabine Mueller, Matthew Dun
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)
