Anti-inflammatory & anti-allergy agents in medicinal chemistry最新文献

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Design of Antiacne Gel Containing Phloretin. 含根皮素抗痘凝胶的设计。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2026-05-15 DOI: 10.2174/0118715230421058251210113310
Manu Sharma, Vibha Kumari, Meenakshi Bajpai
{"title":"Design of Antiacne Gel Containing Phloretin.","authors":"Manu Sharma, Vibha Kumari, Meenakshi Bajpai","doi":"10.2174/0118715230421058251210113310","DOIUrl":"https://doi.org/10.2174/0118715230421058251210113310","url":null,"abstract":"<p><strong>Introduction: </strong>Acne vulgaris is a common and complex skin condition characterised by excess oil production, blocked pores, and inflammatory lesions, such as papules and nodules. While hormonal factors and sebum overproduction are key contributors, the bacterium Staphylococcus aureus has also been recognised as a contributing pathogen. Phloretin, a flavonoid present in plants, like apples, is a promising new compound for acne treatment. Its potential rests in a variety of biological activities beyond merely acting as an antioxidant. Phloretin displays anti-inflammatory and antibacterial properties, which could directly target both the inflammatory response and the bacterial component of acne. These multiple mechanisms of action indicate that a phloretin-based gel could offer a comprehensive solution for managing the condition.</p><p><strong>Materials and methods: </strong>Antiacne gels containing varying concentrations of Carbopol and phloretin were prepared and evaluated. Key parameters included physical appearance, viscosity, pH, drug content, in vitro drug release, and antimicrobial activity against Staphylococcus epidermidis.</p><p><strong>Results: </strong>The optimized hydrogel (F4) exhibited a pH of 6.68, viscosity of 35.9 cP, and drug content of 80.9%. In vitro release studies showed a maximum drug release of 75% over 120 minutes. The formulation displayed strong antimicrobial activity with an inhibition zone of 11 mm, comparable to the marketed benzoyl peroxide gel. The gel was also well tolerated, with no signs of skin irritancy.</p><p><strong>Discussion: </strong>Antiacne gel containing phloretin can be regarded as a more effective treatment for acne. The optimized formulation consisted of phloretin, Carbopol, ethanol, sodium benzoate, PEG 400, propylene glycol, and triethanolamine, showing better results in terms of antimicrobial activity.</p><p><strong>Conclusion: </strong>Phloretin-based gel demonstrated promising antiacne potential, achieving effective drug release and significant antibacterial activity against Staphylococcus epidermidis, while maintaining acceptable physicochemical and dermatological properties.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147985059","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Immunomodulatory Nanocarriers in Multiple Sclerosis: Dual Targeting of Microglia and Mitochondria for Precision Neurotherapy. 免疫调节纳米载体在多发性硬化症:精确神经治疗的小胶质细胞和线粒体双重靶向。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2026-05-15 DOI: 10.2174/0118715230437703251219204750
Ayushi Bhandari, Shikha Baghel Chauhan, Indu Singh, Chirag Jain
{"title":"Immunomodulatory Nanocarriers in Multiple Sclerosis: Dual Targeting of Microglia and Mitochondria for Precision Neurotherapy.","authors":"Ayushi Bhandari, Shikha Baghel Chauhan, Indu Singh, Chirag Jain","doi":"10.2174/0118715230437703251219204750","DOIUrl":"https://doi.org/10.2174/0118715230437703251219204750","url":null,"abstract":"<p><p>The chronic neuroinflammatory and neurodegenerative disease known as Multiple Sclerosis (MS) is characterized by mitochondrial dysfunction and ongoing microglial activation. Developments in nanomedicine have enabled the design of immunomodulatory nanocarriers that target mitochondria and microglia simultaneously, thereby addressing two key pathogenic characteristics. By delivering antioxidants and anti-inflammatory drugs straight to microglia and their mitochondria, these systems increase the effectiveness and specificity of treatment. This review summarizes preclinical research on nanocarriers for delivery to the central nervous system, including liposomes, polymeric nanoparticles, dendrimers, amphiphilic polymer nanoparticles, and modified exosomes, for the years 2020-2025. Functionalized liposomes containing microglia-specific peptides or Toll-like receptor 4 ligands can boost microglial uptake by up to five times, which causes cells to adopt anti-inflammatory characteristics. By incorporating antioxidants such as coenzyme Q₁₀ and N-acetylcysteine, and by using polymeric nanoparticles with mitochondrial- targeting groups, such as triphenyl phosphonium, these nanoparticles improve blood-brain barrier penetration and restore mitochondrial function. Dendrimers and exosomes facilitate effective intracellular and mitochondrial transport, reducing oxidative stress and inflammatory signaling, whereas amphiphilic polymer nanoparticles target scavenger receptors to decrease protein aggregation and neuroinflammation. In MS models, dual-targeting nanocarriers that combine mitochondrial repair and microglial modulation exhibit synergistic neuroprotective effects. Even with promising preclinical findings, there are still obstacles to overcome to achieve clinical translation, scale up production, and ensure long-term safety. Early microglial modulator experiments using sophisticated delivery devices show promise. Finally, dual-targeting immunomodulatory nanocarriers present a new precision neurotherapy strategy for multiple sclerosis. Sustained improvement of clinical pathways, safety, and pharmacokinetics may revolutionize therapeutic approaches and enhance patient outcomes.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147985042","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Polythiophene Nanocomposites as Smart and Sustainable Materials: Advancements in Energy, Environmental, and Biomedical Technologies. 聚噻吩纳米复合材料作为智能和可持续材料:能源、环境和生物医学技术的进展。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2026-05-12 DOI: 10.2174/0118715230407392251102081941
Shikha Baghel Chauhan, Indu Singh, Rohan, Chirag Jain
{"title":"Polythiophene Nanocomposites as Smart and Sustainable Materials: Advancements in Energy, Environmental, and Biomedical Technologies.","authors":"Shikha Baghel Chauhan, Indu Singh, Rohan, Chirag Jain","doi":"10.2174/0118715230407392251102081941","DOIUrl":"https://doi.org/10.2174/0118715230407392251102081941","url":null,"abstract":"<p><p>Polythiophene-based nanocomposites have emerged as a promising class of functional materials due to their tunable electrical conductivity, optical responsiveness, environmental stability, and structural versatility. This review presents a comprehensive analysis of the sustainable synthesis approaches and multifunctional characteristics of polythiophene nanocomposites, emphasizing their potential in smart and environmentally responsive material systems. Various synthesis strategies, including in-situ polymerization, electrochemical deposition, and green chemical oxidation methods, are discussed in the context of enhancing material performance while minimizing ecological impact. The incorporation of nanofillers such as carbon nanotubes, graphene, metal oxides, and layered silicates significantly influences the physicochemical properties of polythiophene matrices, improving conductivity, mechanical strength, thermal resistance, and morphological control. These enhanced features have positioned polythiophene-based nanocomposites as viable candidates for applications in energy storage devices (supercapacitors and batteries), chemical and biosensors, environmental remediation technologies, and biomedical interfaces. Moreover, the review highlights current challenges in scalability, cost-effectiveness, structural stability under operational conditions, and biocompatibility. Limitations related to process control, environmental toxicity of precursors, and long-term material degradation are also acknowledged. Future research directions are proposed to address these barriers, including the development of low-toxicity dopants, recyclable synthesis routes, and computational modelling for material optimization. In summary, polythiophene-based nanocomposites represent a key advancement in smart material development, combining sustainability with multifunctionality. With continued innovation in design and synthesis, they hold significant promise for widespread deployment in industrial and biomedical sectors as part of a greener technological future.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-05-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147978007","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Inhibition of Fenton Reaction-driven Lipid Peroxidation and Anti-inflammatory Activity of Extracts from Roots of Debregeasia Longifolia. 长叶泻根提取物抑制Fenton反应驱动的脂质过氧化及抗炎活性。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2026-04-10 DOI: 10.2174/0118715230437161260331073929
Faruk Alam, Moidul Islam Judder, Sumi Barman, Md Moidul Islam, Mohidul Islam, Atul Adhikari, Sarbanga Bezbaruah
{"title":"Inhibition of Fenton Reaction-driven Lipid Peroxidation and Anti-inflammatory Activity of Extracts from Roots of Debregeasia Longifolia.","authors":"Faruk Alam, Moidul Islam Judder, Sumi Barman, Md Moidul Islam, Mohidul Islam, Atul Adhikari, Sarbanga Bezbaruah","doi":"10.2174/0118715230437161260331073929","DOIUrl":"https://doi.org/10.2174/0118715230437161260331073929","url":null,"abstract":"<p><strong>Introduction: </strong>Debregeasia longifolia has been used traditionally in treating inflammatory and oxidative stress-associated disorders, but the potential of this herb in redox modulation has not been fully defined. Lipid peroxidation in biological substrates sensitive to oxygen acts as a good biomarker to determine antioxidant potential. The objective of this paper was to assess the antioxidant and anti-inflammatory properties of D. longifolia root extracts and to determine the connection between those properties and the levels of polyphenols and flavonoids.</p><p><strong>Methods: </strong>The roots of D. longifolia that were collected in Meghalaya, India, were authentic and extracted sequentially with increased polarity of the solvents. The antioxidant activity was determined by the inhibition of lipid peroxidation of brain lipid substrates by the Fe2+/H2O2 (Fenton reaction)- induced lipid peroxidation through the TBARS technique. Anti-inflammatory activity was assessed through carrageenan-induced swelling of paws in rats and protein denaturation inhibition. The polyphenols and flavonoids were totaled, and correlation analysis was conducted.</p><p><strong>Results: </strong>The lipid peroxidation inhibition of the ethanol extract was the highest (49.55%) and followed by the hydroalcoholic extract (45.17%). Antioxidant activity had strong positive relations with polyphenol (r = 0.9784) and flavonoid (r = 0.9624) contents. Extracts at 250 mg/kg were both found to be effective in reducing carrageenan-induced paw edema and as effective as indomethacin. Phytochemical analysis was performed, identifying compounds such as 2-propylphenol, quercetin glycosides, and atrazine-desethyl.</p><p><strong>Discussion: </strong>The ability to exert strong antioxidant and anti-inflammatory effects is probably due to the high content of polyphenols and flavonoids, which could be mediated by COX-2 and 5-LOX inhibitors.</p><p><strong>Conclusion: </strong>This paper confirms the traditional application of D. longifolia and demonstrates ethanolic root extracts as potential natural antioxidants and anti-inflammatory agents with therapeutic benefits.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-04-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147680134","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Developments in the Management Strategies for Allergy: Advances in Artificial Intelligence and Future Perspectives. 过敏管理策略的发展:人工智能的进展和未来展望。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2026-01-01 DOI: 10.2174/0118715230389406250906142050
Suraj Kumar, Rishabha Malviya, Sathvik Belagodu Sridhar, Javedh Shareef, Tarun Wadhwa
{"title":"Developments in the Management Strategies for Allergy: Advances in Artificial Intelligence and Future Perspectives.","authors":"Suraj Kumar, Rishabha Malviya, Sathvik Belagodu Sridhar, Javedh Shareef, Tarun Wadhwa","doi":"10.2174/0118715230389406250906142050","DOIUrl":"10.2174/0118715230389406250906142050","url":null,"abstract":"<p><strong>Introduction: </strong>Artificial intelligence (AI) is rapidly transforming biomedical research by offering advanced tools to analyse complex datasets. In the field of allergy studies, however, the translation of AI-generated insights into clinical practice remains limited and underutilised.</p><p><strong>Method: </strong>This review critically discussed the current applications of AI in allergy studies. It focuses on the methodological foundations of AI, including machine learning and clustering algorithms, and assesses their practical benefits and limitations. Representative case studies are explored to demonstrate real-world applications, and challenges in data quality, integration, and algorithmic fairness are examined.</p><p><strong>Results: </strong>AI techniques have shown promise in tasks such as disease phenotyping and patient stratification within allergy research. Case studies reveal that AI can uncover immunological insights and support precision medicine approaches. However, the field faces challenges, including fragmented data sources, algorithmic bias, and the limited presence of therapeutic AI tools in clinical practice.</p><p><strong>Discussion: </strong>Despite the demonstrated potential, several barriers hinder the broader adoption of AI in allergy care. These include the need for high-quality, standardised datasets, ethical oversight, and transparent methodologies. The review highlights the importance of these factors in ensuring the reliability, reproducibility, and equity of AI-driven interventions in allergy research.</p><p><strong>Conclusion: </strong>AI holds significant promise for improving diagnostic accuracy and enabling personalised treatment strategies in allergy care. Realising its full potential will require robust frameworks, ethical governance, and interdisciplinary collaboration to overcome current limitations and drive clinical translation.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"15-43"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145083015","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Preface. 前言。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2026-01-01 DOI: 10.2174/0118715230495733260325093041
Claudiu T Supuran
{"title":"Preface.","authors":"Claudiu T Supuran","doi":"10.2174/0118715230495733260325093041","DOIUrl":"10.2174/0118715230495733260325093041","url":null,"abstract":"","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"iii"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147597384","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Pyrazole Derivatives as Selective COX-2 Inhibitors: An Updated Review. 吡唑衍生物作为选择性COX-2抑制剂:最新综述。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2026-01-01 DOI: 10.2174/0118715230435505251027113148
Rajarshi Nath, Bikram Nandi, Arindam Maity, Sourav Maiti, Indrajit Maity, Sourasish Mallick, Shah Alam Khan, Samiran Paul, Biplab Debnath, Md Jawaid Akhtar
{"title":"Pyrazole Derivatives as Selective COX-2 Inhibitors: An Updated Review.","authors":"Rajarshi Nath, Bikram Nandi, Arindam Maity, Sourav Maiti, Indrajit Maity, Sourasish Mallick, Shah Alam Khan, Samiran Paul, Biplab Debnath, Md Jawaid Akhtar","doi":"10.2174/0118715230435505251027113148","DOIUrl":"10.2174/0118715230435505251027113148","url":null,"abstract":"<p><p>Inflammation is a defensive mechanism in the pathophysiology of many chronic diseases, including cancer, gastrointestinal problems, arthritis, cardiovascular disease, chronic wounds, and lesions, which may lead to death worldwide. Research over several decades has resulted in many non-steroidal anti-inflammatory drugs (NSAIDs), but they are associated with adverse drug reactions. As a result, the need for new anti-inflammatory drugs has significantly increased. A key target of NSAIDs, cyclooxygenase (COX) catalyses the synthesis of prostanoids, a broad family of arachidonic acid metabolites including prostacyclin, thromboxane, and prostaglandins. The inhibition of COX is implicated in gastrointestinal toxicities and ulceration. The inducible isoform of COX-2 is quickly expressed in various cell types in response to proinflammatory chemicals, cytokines, growth factors, and diseases related to inflammation. Thus, avoidance strategies for the nonselective COX inhibition and targeting COX-2 selectively are studied for COX-2 inhibitors for the treatment of inflammation, free from side effects. The scaffolds present in known inhibitors are important to achieve the goals. Pyrazole is the most noticeable and familiar heterocyclic scaffold. The prominent anti-inflammatory properties of pyrazole derivatives make them an important family of drugs. This article provides a comprehensive overview of new pyrazole derivatives synthesis and inhibitory activity against COX-2 for the past 5 years. The structure-activity relationship (SAR) and docking insights from this article could be helpful for the medicinal chemist in the development of next-generation COX-2 inhibitors.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"91-106"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147313928","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Anti-inflammatory Potential of Pongamia pinnata: A Comprehensive Review on Molecular Mechanisms and Therapeutic Implications. 桄榔子的抗炎潜能:分子机制和治疗意义的综合综述。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2026-01-01 DOI: 10.2174/0118715230426226260126161153
Bhumika Dudhatra, Kashyap Thummar, Jigna Vadalia, Vaibhav Bhatt
{"title":"Anti-inflammatory Potential of <i>Pongamia pinnata</i>: A Comprehensive Review on Molecular Mechanisms and Therapeutic Implications.","authors":"Bhumika Dudhatra, Kashyap Thummar, Jigna Vadalia, Vaibhav Bhatt","doi":"10.2174/0118715230426226260126161153","DOIUrl":"10.2174/0118715230426226260126161153","url":null,"abstract":"<p><p>Pongamia pinnata (L.) has long been used in both the Ayurvedic and Siddha systems of medicine. It belongs to the leguminous family and shows significant potential for antiinflammatory activity, further supported by growing pharmacological and mechanistic evidence. This paper discusses recent advances in the study of its phytochemistry and the molecular mechanisms underlying its anti-inflammatory effects. Flavonoids, furanoflavonoids, terpenoids, and sterols are the main bioactive compounds, which modulate key inflammatory pathways such as NF- κB, COX-2, iNOS, and the expression of proinflammatory cytokines. Antioxidant, immunomodulatory, and membrane-stabilising activities help reduce oxidative stress and inflammation. Diseasespecific evidence highlights potential roles in arthritis, metabolic inflammation, neurodegeneration, and skin disorders. Emerging formulation approaches, including nanoparticles, ethosomes, and hydrogels, have improved the bioavailability, stability, and targeted delivery of various constituents of P. pinnata. Although preclinical studies have demonstrated a favourable safety profile, inadequate clinical validation and the need for standardised formulations remain two major barriers to therapeutic translation. This review aims to guide future research towards standardisation, pharmacokinetics, and formulation development to position P. pinnata as an attractive candidate for anti-inflammatory drug development.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"189-203"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147629684","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Clinical Applications of Ligand Traps Targeting Activin Type II Receptors. 靶向激活素II型受体的配体陷阱的临床应用。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2026-01-01 DOI: 10.2174/0118715230416604251029062751
Kunihiro Tsuchida
{"title":"Clinical Applications of Ligand Traps Targeting Activin Type II Receptors.","authors":"Kunihiro Tsuchida","doi":"10.2174/0118715230416604251029062751","DOIUrl":"10.2174/0118715230416604251029062751","url":null,"abstract":"<p><p>This review summarizes recent advances in ligand trap therapies targeting activin type II receptors [ActRIIA/ACVR2A and ActRIIB/ACVR2B], which serve as shared receptors for members of the TGF-β family, including activins, GDF11, and myostatin [MSTN]. These receptors mediate Smad2/3 signaling and play critical roles in hematopoiesis, vascular homeostasis, and muscle regulation. Two peptide-based ligand traps have recently received clinical approval: luspatercept [ActRIIB-Fc], an erythroid maturation agent, and sotatercept [ActRIIA-Fc], a novel therapeutic agent for pulmonary arterial hypertension [PAH]. Luspatercept primarily inhibits activin B and GDF11, thereby promoting late-stage erythropoiesis and demonstrating efficacy in anemia associated with conditions such as myelodysplastic syndromes [MDS] and β-thalassemia. Sotatercept binds activins and GDFs to rebalance Smad2/3 and Smad1/5/8 signaling, thereby improving vascular remodeling in PAH. Although both agents have failed to increase skeletal muscle mass in clinical trials consistently, they represent significant advances in the treatment of hematopoietic and vascular disorders. Future studies should focus on optimal dosing strategies, long-term safety, and potential synergistic effects when combined with other therapeutic modalities.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"73-78"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145902179","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design, Spectral Insights, and Enhanced Antioxidant Potential of Novel Phenothiazine Derivatives-1. 新型吩噻嗪衍生物的设计、光谱洞察和增强抗氧化潜力-1。
Anti-inflammatory & anti-allergy agents in medicinal chemistry Pub Date : 2026-01-01 DOI: 10.2174/0118715230378846251009082148
Shamsher Singh, Himanchal Sharma, Smiriti Gohri, Dhananjay Taumer
{"title":"Design, Spectral Insights, and Enhanced Antioxidant Potential of Novel Phenothiazine Derivatives<sup>-1</sup>.","authors":"Shamsher Singh, Himanchal Sharma, Smiriti Gohri, Dhananjay Taumer","doi":"10.2174/0118715230378846251009082148","DOIUrl":"10.2174/0118715230378846251009082148","url":null,"abstract":"<p><strong>Introduction: </strong>Phenothiazine derivatives represent an important class of heterocyclic compounds known for a wide range of pharmacological activities. Their antioxidant potential has drawn considerable interest for therapeutic applications against oxidative stress-related disorders. This study focused on synthesizing a new series of phenothiazine derivatives and evaluating their antioxidant activity.</p><p><strong>Methods: </strong>A series of phenothiazine derivatives [5a-5h] was synthesized by conjugating phenothiazine with various aryl amines via an acetyl linker using standard organic synthesis techniques. The structures of the synthesized compounds were confirmed using spectroscopic techniques, including FT-IR, ^1H NMR, ^13C NMR, and mass spectrometry (MS). Antioxidant activity was assessed using two in vitro assays: the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method and the low-density lipoprotein (LDL) oxidation inhibition assay.</p><p><strong>Results: </strong>All synthesized compounds were successfully characterized by the aforementioned spectroscopic techniques. The antioxidant assays revealed that most of the derivatives exhibited notable antioxidant activity. Among them, Compound 5e, bearing a 4-amino-2-methoxyphenol moiety, demonstrated the highest activity, surpassing the standard antioxidants Vitamin C and butylated hydroxyanisole (BHA). Conversely, compound 5h showed comparatively lower activity.</p><p><strong>Discussion: </strong>The findings indicate that structural variations, particularly the presence of electrondonating groups on the phenothiazine ring, significantly influence antioxidant potential. The superior performance of Compound 5e highlights the importance of specific substituent patterns in enhancing biological activity. However, further investigation into pharmacokinetics and in vivo efficacy is necessary to support potential therapeutic use.</p><p><strong>Conclusion: </strong>The study successfully synthesized and characterized a novel series of phenothiazine derivatives, several of which exhibited potent antioxidant properties. Structure- activity relationship (SAR) analysis suggested that electron-donating substituents enhance activity, pointing to promising future applications in treating oxidative stress-related conditions.</p>","PeriodicalId":94368,"journal":{"name":"Anti-inflammatory & anti-allergy agents in medicinal chemistry","volume":" ","pages":"107-128"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145902158","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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