Mini reviews in medicinal chemistry最新文献

{"title":"Phytochemical and Biological Biodiversity of Tomato (Solanum lycopersicum L.) (2010-2022).","authors":"Marwa A M Abdel-Razek, Miada F Abdelwahab, Usama Ramadan Abdelmohsen, Ashraf N E Hamed","doi":"10.2174/0113895575347047250506102300","DOIUrl":"https://doi.org/10.2174/0113895575347047250506102300","url":null,"abstract":"<p><p>Tomato (Solanum lycopersicum L.) is one of the most common vegetable plants in the world. It is also named Lycopersicon esculentum. It serves as a model plant for the Solanaceae family, especially for plants that produce fleshy fruits. Various studies have shown that S. lycopersicum fruits, seeds, leaves, roots, in addition to tomato waste, constitute sources of vital bioactive substances such as lycopene, flavonoids, vitamins, and minerals. Consequently, tomatoes have powerful antioxidant activities in addition to cardiovascular protection, anticancer, antimutagenic, antiinflammatory, antimicrobial, neuroprotective, antidiabetic, radioprotective, gut modulating activities, vision effect, and hepatoprotective. The current review illuminates the different isolated phytochemicals and medicinal value, as well as the pharmacological activities of S. lycopersicum.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143972100","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Recent Developments in Triazole Derivatives as α-Glucoside Inhibitors for the Treatment of Diabetes.","authors":"Priya Devi, Subhadip Maity, Shankar Gupta, Aastha Singh, Sant Kumar Verma, Vivek Asati","doi":"10.2174/0113895575371876250429175826","DOIUrl":"https://doi.org/10.2174/0113895575371876250429175826","url":null,"abstract":"<p><p>Diabetes mellitus, a serious metabolic health condition and one of the most common diseases around the globe, primarily arises due to elevated blood sugar levels and causes multiple metabolic abnormalities. Nowadays, it has become the biggest challenge for the scientific community. Serious fatal health problems, such as neuropathy, retinopathy, and nephropathy, are the result of mismanagement of this illness, which significantly lowers the quality of life. α-glucosidase is an enzyme in the small intestine that causes the breakdown of complex polysaccharide units into glucose units, i.e., smaller units that then enter the bloodstream and result in hyperglycaemic conditions. To solve this issue, the inhibitors of α-glucosidase must be developed immediately to manage and treat diabetes in patients. This literature survey highlights the importance of triazoles containing different heterocyclic rings, such as furan, benzyl, benzimidazole, thiazole, pyrrole, coumarin, indole, xanthone, etc., which have shown promising antidiabetic activity against α-glucosidase. The parameters, such as kinetic investigations, binding interactions, IC50 value, structure-activity relationship, and molecular docking studies of the most potent compound, are covered in this review, which provides an overview of enzyme inhibitory activity. This review also includes the patents on α-glucosidase with triazole rings, demonstrating their effectiveness against α-glucosidase.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-05-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143971414","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Recent Advances in Small Molecular PET Tracers for Pancreatic Cancer Diagnosis: Preclinical Stage.","authors":"Meijie Pan, Qiusong Chen, Shaobo Yao","doi":"10.2174/0113895575375382250408143606","DOIUrl":"https://doi.org/10.2174/0113895575375382250408143606","url":null,"abstract":"<p><p>Pancreatic cancer [PCa] has a high mortality rate, and early and precision detection is vital to improve the survival rate of PCa. However, current imaging modalities such as ultrasound, CT, MRI, and 18F-FDG PET/CT are limited in diagnosing distant metastatic lesions and specific visualization. In recent years, small molecule tracers targeting tumor stroma or antigens have made significant progress in preclinical applications for preoperative PCa diagnosis and image-guided intraoperative resection. Tracers targeting integrins [avb6] in tumor stroma and NTR1 in tumor antigens have been undergoing clinical safety validation. This review summarized small-molecule radioactive probes targeting tumor stroma or antigens in PCa, evaluated their imaging characteristics, clinical potential, and the advantages of multi-targeted probe combinations. Additionally, it explored the potential of novel probes for fluorescence imaging-guided intraoperative resection.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144007168","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Innovative Theranostics Strategies in the Fight Against Lung Cancer.","authors":"Aashi Jain, Sakshi Soni, Vandana Soni, Sushil Kumar Kashaw","doi":"10.2174/0113895575338753250228055700","DOIUrl":"https://doi.org/10.2174/0113895575338753250228055700","url":null,"abstract":"<p><p>This review delves into the potential of nanotechnology for improved lung cancer diagnosis and treatment. A critical focus is placed on various overexpressed biomarkers within lung tumors. These biomarkers serve as potential targets for nanoparticle-based drug delivery strategies. The review explores two main targeting approaches: passive and active (receptor-based) targeting. Active targeting mechanisms like EGFR, folic acid, and CD44 receptor targeting are specifically discussed. Additionally, the review examines stimuli-responsive systems for targeted drug delivery, including pH, temperature, ligand-attached, and multi-stimuli-responsive systems. Moreover, the role of nanotechnology in theranostics, which combines therapeutic and diagnostic capabilities, is explored and different types of nanocarriers, including lipid-based, polymer-based, metal-based, and magnetic nanoparticles, are examined for their potential applications. The review also highlights advancements in lung cancer diagnostic techniques beyond nanotechnology. This includes emerging tools like biomarkers, biosensors, and artificial intelligence, alongside improvements to established methods. Finally, the review provides a glimpse into ongoing clinical trials and concludes by emphasizing the transformative potential of nanotechnology in improving lung cancer patient outcomes.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143586292","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Innovative Horizons in Drug Design: Exploring the Synthesis and Medicinal Properties of Heterocyclic Schiff Bases. A Review.","authors":"Yousaf Khan, Hina Sarfraz, Wajid Rehman, Momin Khan, Liaqat Rasheed, Khursheed Ur Rahman","doi":"10.2174/0113895575320413250126041041","DOIUrl":"https://doi.org/10.2174/0113895575320413250126041041","url":null,"abstract":"<p><p>Schiff bases are an important scaffold for designing drug development. They are characterized by having a carbon-nitrogen double bond. This double bond is synthesized by different synthetic schemes by both the aromatic and aliphatic chains. Bases inspired chemists due to their versatile importance in drug discovery and drug development. A large number of drugs are designed through the heterocyclic Schiff base moieties. This review highlighted the importance of Schiff bases concerning their bioactive importance in drug design. Moreover, amide-iminol tautomerism is a significant tool for the high biological importance of Schiff bases due to the presence of the C=N bond. Furthermore, the reported synthesized heterocyclic scaffolds Schiff bases have a wide range of biological importance. Due to this different biological importance, such as antimicrobial, anticonvulsant, analgesic, antioxidant, antimalarial, anti-inflammatory, anticancer, antidiabetic, and antileishmanial properties, the researcher has shown their interest by synthesizing different heterocyclic Schiff bases. In this review article, biologically active heterocyclic Schiff bases were reviewed intensively concerning drug design and drug development.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-02-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143516080","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Effects of Antioxidant Approved Drugs and Under Investigation Compounds with Potential of Improving Sleep Disorders and their Associated Comorbidities associated with Oxidative Stress and Inflammation.","authors":"Panagiotis Theodosis-Nobelos, Fani-Niki Varra, Michail Varras, Eleni A Rekka","doi":"10.2174/0113895575360959250117073046","DOIUrl":"https://doi.org/10.2174/0113895575360959250117073046","url":null,"abstract":"<p><p>Sleep disorders and the resultant sleep deprivation (SD) are very common nowadays, resulting in depressed mood, poor memory and concentration, and various important changes in health, performance and safety. They may provoke further impairment of the cell lining of the blood vessels, as acting as a risk factor for cardiovascular disease (CVD) onset and progression. SD may lead to low neuronal regaining and plasticity, drastically affecting brain function. Thus, SD is a known risk factor for mental, behavioral and developmental disorders. Due to the inflammatory and oxidative stressful nature of SD, immune response modulation and antioxidants could be another therapeutic approach, apart from the already known symptomatic treatment with sedatives. Additionally, many drugs approved for other indications and under investigation, have been revisited due to their wide array of pharmacological activities. This review summarizes the main aspects of SD pathology and SD interrelated comorbidities and presents direct and indirect antioxidant molecules and drugs with multi-targeting potential that could assist in the prevention or management of these factors. A number of research groups have investigated well-known antioxidant compounds with multi-targeting cores, combining structural characteristics with properties including antiinflammatory, metal chelatory, gene transcription and immune modulatory that may add towards the effective SD and its associated comorbidities treatment.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-02-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143432838","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"In vivo Pharmacokinetic and ADMET Profiles of Synthetic Antimicrobial Peptides (AMPs): A Review.","authors":"Muhammad Akram Mohd Noordin, Ahmed Abdulkareem Najm, Herryawan Ryadi Eziwar Dyari, Douglas Law, Sharifah Sakinah Syed Alwi, Azwan Mat Lazim, Yew Hoong Cheah, Thiam Tsui Tee, Shazrul Fazry","doi":"10.2174/0113895575362479241231054240","DOIUrl":"https://doi.org/10.2174/0113895575362479241231054240","url":null,"abstract":"<p><p>The broad-spectrum action and capacity to target drug-resistant infections make synthetic Antimicrobial Peptides (AMPs) popular therapeutic agents. Indeed, the effective use of these peptides in clinical application relies on a thorough understanding of their Pharmacokinetic (PK) and ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) characteristics. Despite growing research on synthetic AMPs, there is a notable gap in the literature specifically addressing their ADMET profiles. Previous reviews have not extensively covered this area, providing a vital opportunity to study synthetic AMPs' pharmacokinetics and safety, which are crucial for their therapeutic development. This review covered research studies that focused on PK and ADMET of synthetic antimicrobial peptides from several databases, including Google Scholar, SCOPUS, PubMed, and Science Direct, within the years 2020 to 2024, and 12 related research papers have been found. AMPs display a wide range of PK behaviors, including rapid renal clearance, liver-centric distribution, broad distribution with low toxicity, high kidney retention, and gradual absorption with dose-dependent toxicity. Overall, the ADMET profiles of AMPs are crucial in assessing their therapeutic potential, and continuous study is necessary to enhance their practical feasibility. An in-depth investigation of the in vivo ADMET and pharmacokinetic profiles of synthetic AMPs is presented in this review to address the current gap in the research. The findings of this study provide important insights for developing synthetic AMPs as effective antimicrobial drugs.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143414539","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Role of Renin-Angiotensin System in Diabetic Nephropathy: An Update.","authors":"André Sanglard, Bárbara Castello Branco Miranda, Ana Luiza França Vieira, Marcus Vinicius Miranda Macedo, Rodrigo Lara Santos, Aléxia Stenner Rodrigues Radicchi Campos, Amanda Campos Piva, Ana Cristina Simões E Silva","doi":"10.2174/0113895575344980250130062547","DOIUrl":"https://doi.org/10.2174/0113895575344980250130062547","url":null,"abstract":"<p><strong>Background and aims: </strong>Diabetic nephropathy (DN) is an important complication of diabetes, leading to end-stage renal disease (ESRD) worldwide. This review aimed to explore the role of the renin-angiotensin system (RAS) in DN, highlighting current treatments and emerging therapeutic perspectives.</p><p><strong>Methods: </strong>We conducted a narrative review of the literature up to March 2024, focusing on the classical and alternative RAS axes, their implications in DN, and novel therapeutic approaches. Data were sourced from Scopus, PubMed, Scielo, and Cochrane databases.</p><p><strong>Results: </strong>The classical RAS axis, involving angiotensin-converting enzyme (ACE), Angiotensin II (Ang II), and the AT1 receptor, promotes vasoconstriction, sodium retention, and fibrosis in DN. Hyperglycemia-induced Ang II increases oxidative stress, contributing to glomerular hyperfiltration and kidney damage. Current treatments include ACE inhibitors and angiotensin receptor blockers (ARBs), which reduce blood pressure and proteinuria, delaying DN progression. In contrast, the alternative RAS axis, featuring ACE2, Ang-(1-7), and the Mas receptor, offers renoprotective effects by counteracting Ang II actions. Ang-(1-7) reduces inflammation, fibrosis, and podocyte apoptosis. ACE2 activators, Ang-(1-7), and Mas receptor agonists show promise in preclinical studies, reducing glomerular fibrosis and improving renal function. Ang-(1-9) and alamandine may also hold potential in future treatments. Emerging therapies, such as the SGLT2 inhibitors, also demonstrate benefits in reducing DN progression.</p><p><strong>Conclusion: </strong>While ACE inhibitors, ARBs, and SGLT2 inhibitors remain central to DN management, the ACE2-Ang-(1-7)-Mas axis presents a promising therapeutic target. Future research should focus on translating preclinical findings into clinical applications, potentially improving DN treatment.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143399473","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Application of the Pyrazole Structure in the Structural Modification of Natural Products.","authors":"Fu-Qun Sun, Ya-Lan Wang, Ke Sun, Fei-Xia Yue, Yun-Xia Sun, Jia-Hong Ju, Zhan-Hui Jin, Qing-Kun Shen, Hong-Yan Guo, Mei-Hui Liu, Zhe-Shan Quan","doi":"10.2174/0113895575359419241211092252","DOIUrl":"https://doi.org/10.2174/0113895575359419241211092252","url":null,"abstract":"<p><p>Most natural products in nature have broad but not exceedingly good biological activities. The pyrazole structure has been introduced into natural products due to its suitability for various synthetic methods and its broad pharmacological activities. This article provides a detailed introduction to the anti-inflammatory, antibacterial, antifungal, antiviral, and anti-Alzheimer disease activities of pyrazole-modified natural product derivatives, particularly their anti-tumor activity. It is worth noting that compared to lead compounds, most natural product derivatives modified with pyrazole exhibit excellent pharmacological activity. Some of these derivatives exhibit outstanding anti-tumor activity, with IC50 values reaching nanomolar levels. This review provides more research directions and choices for future studies on natural products.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-01-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143033554","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Drug Repurposing: A Conduit to Unravelling Metabolic Reprogramming for Cancer Treatment.","authors":"Shristy Chaudhary, Abhilash Rana, Seema Bhatnagar","doi":"10.2174/0113895575339660250106093738","DOIUrl":"https://doi.org/10.2174/0113895575339660250106093738","url":null,"abstract":"<p><p>Metabolic reprogramming is a hallmark of cancer. Distinct and unusual metabolic aberrations occur during tumor development that lead to the growth and development of tumors. Oncogenic signaling pathways eventually converge to regulate three major metabolic pathways in tumor cells i.e., glucose, lipid, and amino acid metabolism. Therefore, identifying and targeting the metabolic nodes of cancer cells can be a promising intervention and therapeutic strategy for patients with malignancies. The long road of new drug discovery for cancer therapy has necessitated relooking alternative strategies such as drug repurposing. Advanced genomic and proteomic technologies for the assessment of cancer-specific biological pathways have led to the discovery of new drug targets, which provide excellent opportunities for drug repurposing. The development of effective, safe, cheaper, and readily available anticancer agents is the need of the hour, and drug repurposing has the potential to break the current drug shortage bottleneck. This review will accordingly cover various metabolic pathways that are aberrant in cancer, and strategies for targeting metabolic reprogramming by using repurposed drugs.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143008278","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}