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Current Topics in Medicinal Chemistry - Online First
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21 - 40 of 46 results
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Roles of C/EBPβ/AEP in Neurodegenerative Diseases
Authors: Jing Guo, Xin-Yi Liu, Sha-Sha Yang, Qiang Li, Yang Duan, Shan-Shan Zhu, Ke Zhou, Yi-Zhi Yan and Peng ZengAvailable online: 27 January 2025More LessIn recent years, an increasing number of studies have shown that increased activation of aspartic endopeptidases (AEPs) is a common symptom in neurodegenerative diseases (NDDs). AEP cleaves amyloid precursor protein (APP), tau (microtubule-associated protein tau), α-synuclein (α-syn), SET (a 39-KDa phosphoprotein widely expressed in various tissues and localizes predominantly in the nucleus), and TAR DNA-binding pro Read More
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SRT1720 Treatments Hepatic Ischemia Reperfusion Injury by Regulation of NF-κB Signaling Pathways and Reduce Cell Apoptosis: From Network Pharmacology to Experimental Validation
Authors: Zhongzhe Li, Wenting Geng, Beilei Yu, Bin Wang, Shuxuan Sun and Lu ZhouAvailable online: 21 January 2025More LessBackground and objective Hepatic ischemia reperfusion injury (HIRI) is a common complication closely related to the prognosis of liver surgery, and effective treatment methods are still unavailable. SRT1720 has the characteristics of multifunction and multitarget which may cope with the multidirectional complex pathological process caused by HIRI. The present study aimed to explore the potential mechanism of SRT1720 Read More
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Osseointegration Process Improving via Functionalization of Titanium Dioxide Nanotubes: A Bibliometric Analysis and Systematic Review
Available online: 21 January 2025More LessIntroduction/Objectives Failures of osseointegrated implants pose a significant challenge in the medical field, often attributed to prolonged osseointegration periods and bacterial infections. Functionalization of Titanium Dioxide Nanotubes (TNTs) has emerged as a promising strategy to improve osseointegration and mitigate infections. This study aims to conduct a bibliometric analysis and systematic review to identify tr Read More
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Advances in the Study of Halogenated Natural Products
Authors: Lijing Zhang, Bing Liu, Ting Zhu, Xue Tian, Ning Chen and Yuxin WangAvailable online: 21 January 2025More LessHalogenated natural products are an important class of secondary metabolites that are widely distributed in nature. The presence of halogen atoms usually enhances the pharmacological activity of the compounds. As a result, halogenated natural products have shown promising pharmacological activities in antibacterial, antitumour, anti-inflammatory and antiplasmodial properties, providing a rich resource for th Read More
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Synthesis, X-Ray Structure, Characterization, Antifungal Activity, DFT, and Molecular Simulation of a Novel Pyrazole Carboxylic Acid
Available online: 21 January 2025More LessBackground The search for new antifungal agents is critical due to the rising resistance of fungal pathogens to existing treatments. This study focuses on the synthesis and evaluation of a novel compound, 1-benzyl-5-methyl-1H-pyrazole-3-carboxylic acid (compound L1), as a potential antifungal agent. Methods Compound L1 was synthesized and characterized using a range of analytical techniques, including 1H^1H1H Read More
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Exploring the Therapeutic Potential of Natural Flavonoids in Inflammatory Bowel Disease: Insights into Intestinal Mucosal Barrier Regulation
Authors: Min Wang, Yanqing Zhang, Yaxin Li, Mengyu Zhang, Jinrui Liu, Yuxin Cao, Junbo Xie and Shuo WangAvailable online: 15 January 2025More LessInflammatory Bowel Disease (IBD) is a chronic non-specific disease that affects the gastrointestinal tract, and Intestinal Mucosal Barrier (IMB) damage is closely related to its pathogenesis. The management of IBD often involves repairing the mechanical, chemical, immune, or biological barriers of the intestinal mucosa to alleviate symptoms. Currently, the treatment of IBD patients requires continuous medication or surgi Read More
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100 Years of Insulin: A Historical Perspective
Available online: 10 January 2025More LessBackground Diabetes mellitus, a metabolic disease characterized by high blood glucose levels, has increased dramatically in recent years, prompting the need for more affordable diagnoses and treatments. Objective This study aimed to conduct a brief historical and theoretical review on the development of insulin. Methods Scientific and technological data have been retrieved and analyzed with a focus on the develop Read More
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Synthetic Strategies for the Development of Ibuprofen Derivatives: A Classified Study
Authors: Kuchana Madhavi and Barla Karuna DeviAvailable online: 10 January 2025More LessIbuprofen, a widely used NSAID from the aryl propionic acid class, effectively relieves pain, fever, and inflammation. On prolonged use, it leads to gastrointestinal, hepatic, and renal toxicities, particularly gastrointestinal ulcers. These side effects are largely attributed to the carboxylic acid functional group common to NSAIDs. The present review highlights the different modifications done to the carboxylic group in Ibuprofen Read More
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Targeting Malaria's Achilles' Heels: A Review of Plasmodium Life Cycle Vulnerabilities for Drug Discovery
Authors: Shruti Shukla, Shikha Kushwah and Ashutosh ManiAvailable online: 10 January 2025More LessThe global rise of drug-resistant malaria parasites is becoming an increasing threat to public health, emphasizing the urgent need for the development of new therapeutic strategies. Artimisinin-based therapies, once the backbone of malaria treatment, are now at risk due to the resistance developed in parasites. The lack of a universally accessible malaria vaccine exacerbates this crisis, underscoring the need to Read More
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Conformation Study and Design of Novel 6-Hydroxybenzothiazole-2-Carboxamides as Potentially Potent and Selective Monoamine Oxidase B Inhibitors for Neuroprotection
Authors: Dong Xie, Penghang Guo, Quantang Zhao, Yu Gao, Jianan Zhang and Jie ZhouAvailable online: 10 January 2025More LessBackground 6-hydroxybenzothiazole-2-carboxamide is a novel, potent, and specific monoamine oxidase B inhibitor that can be used to study the structure of molecules and come up with new ways to protect neurons. Objective The objective of this work was to create an effective model using derivatives of 6-hydroxybenzothiazole-2-carboxamide and establish a dependable predictive foundation for the development of neuropr Read More
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Traditional Chinese Medicine for Liver Cancer Treatment: Network Pharmacology Research
Authors: Shihao Zheng, Yixiao Gu, Wenying Qi, Wei Wang, Xiaoke Li, Xiaobin Zao, Size Li, Shaoyu Liu, Tianyu Xue, Yongan Ye and Aimin LiuAvailable online: 09 January 2025More LessBackground As one of the common malignant tumors nowadays, liver cancer has more risk factors for its development and is characterized by a high recurrence rate, high mortality rate, and poor prognosis, which poses a great threat to people's health. The specific efficacy of traditional Chinese medicine is based on clinical practice, which is a high degree of generalization of the characteristics and scope of the clinical eff Read More
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Bioanalysis, Analysis, Chemistry, and Pharmacological Aspects of Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors
Authors: Sunidhi Jain, Roshani Patil and Sanjay SharmaAvailable online: 08 January 2025More LessThe development of Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIF-PHIs), such as Roxadustat (ROX), Enarodustat (ENA), Desidustat (DES), Vadadustat (VAD), Molidustat (MOL), and Daprodustat (DAP), has significant effects on anemia in chronic kidney disease. This review presents comprehensive information about the synthesis, pharmacology, and analysis of HIF-PHIs across several matrices. The literatur Read More
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Benzimidazole Derivatives in Breast Cancer: Target-Specific Therapeutic Breakthroughs
Available online: 07 January 2025More LessDespite ongoing advancements in drug design and developments, breast cancer remains a serious and devastating disease and is ranked as the second most common illness in women. Breast cancer rates have increased significantly during the last 40 years. This necessitates the development of novel treatment techniques. Currently, chemotherapy is the primary mode of treatment for breast cancer; however, its Read More
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Design and Synthesis of 1-(4-Bromo-2-(Pyrrolidine-1-Yl) Benzyl) Piperidine-Based Derivatives as Anti-Tubulin Agents
Authors: Rambabu Guguloth and Shiva Kumar GubbiyappaAvailable online: 02 January 2025More LessBackground Piperidines are among the essential synthetic fragments for designing drugs and play a significant role in the pharmaceutical industry. The synthesis of newer derivatives by incorporating different amines paves the way for the introduction of novel drug combinations for current cancer treatments. Method The new combinations of 1-(4-bromo-2-(pyrrolidine-1-yl) benzyl) piperidine derivatives were synthesized by Read More
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Impact of Copper(II) and Silver(I) Complexes Containing 1,10-Phenanthroline-5,6-dione on Cellular and Virulence Aspects of Scedosporium apiospermum
Available online: 01 January 2025More LessBackground Scedosporium apiospermum is a multidrug-resistant filamentous fungus that causes localized and disseminated diseases. Our group has previously described that metal-based complexes containing copper(II) or silver(I) ions complexed with 1,10-phenanthroline-5,6-dione (phendione) inhibited the viability of S. apiospermum conidial cells. Objective The effects of these promising complexes, [Cu(phendione) Read More
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Neuroactive Phytoconstituents of Glycyrrhiza glabra for the Treatment of Alzheimer’s Disease
Authors: Mansi Verma, Mohd Usman and Niraj Kumar SinghAvailable online: 26 December 2024More LessAlzheimer’s Disease (AD), a prevalent neurodegenerative disorder, poses a significant global health challenge with complicated pathogenesis. Pathological characteristics of AD include increasing loss of cholinergic neurons, oxidative stress, mitochondrial dysfunction, and amyloid beta accumulation. Due to the limited availability of effective therapeutic options with only symptomatic relief and their severe adverse effect Read More
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Thymol-Loaded Zinc Ferrite Nanoparticles: A Novel Carrier for Enhanced Antimicrobial and Antibiofilm Activity against M. smegmatis through ROS-Mediated Mechanism
Available online: 16 December 2024More LessIntroduction/Objective Tuberculosis (TB) remains a persistent global health challenge, with an increasing incidence of cases and limitations in current treatment strategies. Traditional therapy involves long drug treatments that can cause side effects and lead to drug-resistant strains, making treatment less effective. This study aimed to explore the therapeutic potential of a novel nanoparticle-based delivery system for Read More
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Strategies in Parkinson's Disease Therapeutics - A Need for Synergy of Ayurveda, Small Molecules and Nanoparticles aided Approaches
Available online: 27 November 2024More LessDespite extensive research, there is an unmet need for developing disease-modifying therapies for Parkinson’s disease (PD). Failure of certain landmark clinical trials has highlighted the need for a better understanding of the disease pathogenesis as well as identifying the hurdles in developing drug candidates and designing clinical trials. While adhering to these needs, several promising trials are currently underway Read More
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Computer-aided Drug Discovery of Epigenetic Modulators in Dual-target Therapy of Multifactorial Diseases
Authors: Slavica Oljacic, Marija Popovic-Nikolic, Brankica Filipic, Zarko Gagic and Katarina NikolicAvailable online: 04 November 2024More LessNumerous studies suggest that common genetic and epigenetic factors such as p53, histone deacetylase (HDAC), brain-derived neurotrophic factor (BDNF), the (Ataxia Telangiectasia mutated) ATM gene, cyclin-dependent kinase 5 (CDK5), glycogen synthase kinase 3 (GSK3) and altered expression of microRNA (miRNA) play a crucial role in cancer and neurodegeneration. As there is growing evidence that epigenetic aber Read More
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Triazole scaffold-based DPP-IV Inhibitors for the management of Type-II Diabetes Mellitus: Insight into Molecular Docking and SAR
Available online: 31 October 2024More LessDiabetes mellitus, characterized as a chronic metabolic disorder or a polygenic syndrome; is increasing at a very fast pace among every group of the population worldwide. It arises due to the inability of the body to produce enough insulin (the hormone responsible for controlling blood sugar levels) or inability to utilize the insulin, leading to hyperglycaemic condition, which, if left uncontrolled gives rise to chronic microvascular Read More
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