European Journal of Medicinal Chemistry Reports最新文献

{"title":"Hydroxyapatite–polymer nanocomposites for drug delivery applications: A mini review","authors":"Farnaz Behmagham ,&nbsp;Shahad Mohammed Dhiaa ,&nbsp;Abbas Hameed Abdul Hussein ,&nbsp;Usama Kadem Radi ,&nbsp;Hiba Mushtaq ,&nbsp;Ameer Hassan Idan ,&nbsp;Esmail Vessally","doi":"10.1016/j.ejmcr.2024.100231","DOIUrl":"10.1016/j.ejmcr.2024.100231","url":null,"abstract":"<div><div>Prescribing drugs in a traditional way causes drug resistance and side effects. New strategies are being developed to solve these problems and to deliver drugs safely and efficiently to damaged tissues. Drug delivery systems are one of the successful strategies for delivering drugs to the disease site in the body. Hydroxyapatite (HA) due to its similarity to the compositional of bone and tooth and biocompatibility has received more attention in biomedical applications. Nonetheless, its applications are restricted by lower mechanical potency, low colloidal stability, and uncontrolled drug release. The composition of HA with polymers removes its defects as a drug delivery system. Hence, this paper provides clear information on the latest Hydroxyapatite nanocomposites (HAP-PNs) improvements as drug delivery systems. So, it supplies a precise insight into the various synthesis methods of HAp-PNs and newly developed nanocarriers from HAp-PNs. Moreover, this review confers HAp-PNs nanocarrier's possible usage and restrictions in different fields of medicine.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100231"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142532744","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fabrication, characterization and transdermal properties of double cross-linked gel beads with 4-n-butylresorcinol","authors":"Faxin Zhang ,&nbsp;Mengsi Yin ,&nbsp;Wanhui Shao ,&nbsp;Xinyi Li ,&nbsp;Hongmen Ren ,&nbsp;Xianglong Wang ,&nbsp;Mengju Xu ,&nbsp;Qianchan Pang ,&nbsp;Yan Cheng ,&nbsp;Jianjun Xue ,&nbsp;Haijie Hu ,&nbsp;Mingyuan Li","doi":"10.1016/j.ejmcr.2024.100232","DOIUrl":"10.1016/j.ejmcr.2024.100232","url":null,"abstract":"<div><div>In this paper, sodium alginate (SA) -agarose double cross-linked gel beads were prepared to improve the solubility of 4-n-butylresorcinol and to reduce skin irritation. The wrappage material suitable for 4-nBR gel beads was SA-agarose double cross-linking material, and the internal inclusions were in the form of 4-n-butylresorcinol nanoemulsions (4-nBR NEs). Under the orthogonal fluorescence microscope, it was observed that the gel beads were spherical in shape, with smooth and rounded surfaces and permeable interiors. The encapsulation rate of the gel beads was 84.37 ± 3.56 %, and the average diameter was 1.93 ± 0.21 mm. Scanning electron microscopy showed that the gel beads were spherical in shape. The cumulative leakage rate of the gel beads on the 35 th day was 4.72 ± 0.06 %, suggesting that the gel beads encapsulated 4-butylresorcinol to good effect and with high stability. This proves that the gel beads wrapped with 4-nBR are highly effective and stable. <em>In vitro</em> skin permeability assessment verified the good skin permeability of nanoemulsions (NEs).</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100232"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142579016","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design, synthesis, molecular dynamics studies and biological evaluations of 4-hydroxy-5-pyrrolinone-3-carbohydrazides as HIV-1 integrase inhibitors","authors":"Nafiseh Karimi ,&nbsp;Amirreza Dowlati Beirami ,&nbsp;Rouhollah Vahabpour Roudsari ,&nbsp;Zahra Hajimahdi ,&nbsp;Afshin Zarghi","doi":"10.1016/j.ejmcr.2024.100208","DOIUrl":"10.1016/j.ejmcr.2024.100208","url":null,"abstract":"<div><p>Acquired immune deficiency syndrome (AIDS) diseases despite the efficacy of anti-HIV therapy, remain one of the human's most serious problems. Hence, the introduction of novel anti-HIV agents as first-line therapy is still required. HIV integrase lacking human enzyme homologous is an interesting target for developing new anti-HIV drugs. Following our attempts to describe active integrase inhibitor structures, here a series of novel 4-Hydroxy-5-pyrrolinone-3-carbohydrazides as HIV integrase inhibitor agents were identified. Biological results showed that all compounds could inhibit integrase strand transfer reaction and also exhibited anti-HIV activity in a cell-based assay. The interaction between integrase and designed compounds was investigated using molecular docking and molecular dynamics simulations.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100208"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000803/pdfft?md5=e9b5e1971d09654fd918e70450d89bc0&pid=1-s2.0-S2772417424000803-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142039843","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design, synthesis, characterization and antidiabetic evaluation of 3,5-substituted thiazolidinediones: Evidenced by network pharmacology, Molecular docking, dynamic simulation, in vitro and in vivo assessment","authors":"Shankar Gharge,&nbsp;Shankar G. Alegaon,&nbsp;Swaroop Jadhav,&nbsp;Shriram D. Ranade,&nbsp;Rohini S. Kavalapure","doi":"10.1016/j.ejmcr.2024.100213","DOIUrl":"10.1016/j.ejmcr.2024.100213","url":null,"abstract":"<div><p>In search of new antidiabetic agents, heterocyclic compounds containing 3,5-Substituted thiazolidinedione moieties were synthesized through a concise three-step reaction process. The synthesis involved Knoevenagel condensation at the 5th position of the 3,5-Substituted thiazolidinedione ring-system (6a-6c). Comprehensive physicochemical and spectral analyses, including FTIR, HR-MS, ¹H NMR and ¹³C NMR, were performed to characterize the synthesized compounds. The synthesized derivatives were subjected to evaluation for their <em>In vivo</em> anti-diabetic activity against diabetes induced wistar rats and <em>In vitro</em> activity against <em>α-amylase, α-glucosidase</em> and glucose uptake by yeast cells. On the basis of the combined results of network pharmacology<em>, In vitro</em> and animal study experiments revealed that the compounds 6c predicted to have the greatest effect out of the compounds (6a-6c), showing interactions with targets exhibited potential binding patterns against the active site of target <em>α-amylase, α-glucosidase</em> with modulating <em>AMY2A, GAA, PPARG, PIK3CA, PRKCB, INSR,</em> and <em>PRKCB</em> signalling pathways and this is evidenced by molecular docking, dynamics simulation (MD) studies. Further, compound 6c showed <em>In vitro α-amylase, α-glucosidase</em> inhibitory activity with IC₅₀ value of 86.06 ± 1.1 μM and 74.97 ± 1.23 μM as opposed to standard acarbose (IC₅₀ value of 26.89 ± 3.12 and 29.25 ± 0.15 μM) and 58.23 ± 0.13 % of glucose uptake and also exhibited significant reduction (p &lt; 0.001) in blood glucose levels (114 ± 1.17 mg/dL) comparable to the effect of pioglitazone (102.2 ± 0.79 mg/dL). The present study suggests that modified thiazolidinediones act as potential lead compounds to carter the need of antidiabetic agents.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100213"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000852/pdfft?md5=6937eab5d75386afd4b218c9aad7de7a&pid=1-s2.0-S2772417424000852-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142167391","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Progression in nano-botanical oral hygiene solutions: The Dawn of biomimetic nanomaterials","authors":"Aqsa Arif ,&nbsp;Muhammad Sharif Khar ,&nbsp;Nariman Shahid ,&nbsp;Waqar Aman ,&nbsp;Joham Javed ,&nbsp;Amina Rubab ,&nbsp;Mashal Nayab ,&nbsp;khadija mastoor ,&nbsp;Rabia Arshad ,&nbsp;Abbas Rahdar ,&nbsp;Sonia Fathi-karkan ,&nbsp;Zelal Kharaba ,&nbsp;Sadanand Pandey","doi":"10.1016/j.ejmcr.2024.100219","DOIUrl":"10.1016/j.ejmcr.2024.100219","url":null,"abstract":"<div><div>Pathogenic bacteria consistently pose significant challenges within the oral mucosal environment by altering bioflora, biofilm development, and enamel demineralization, thus leading to extensive clinical resources for treatment. This review aims to gather suitable and novel information in terms of providing advanced bio-inspired therapeutic facilities to alleviate the burden of treatment on both the patient and medical infrastructure. Botanical nanoparticle-based mouthwashes have been synthesized using mostly green synthesis technology. Botanical nanoformulations-based mouthwashes are efficient for maintaining microbial flora and mimicking natural extracellular matrix (ECM) components. Furthermore, dental caries can also be treated by these nanoparticles through the promotion of enamel remineralization and bacterial growth suppression. These nature-inspired oral rinses/mouthwashes confer significant advantages relative to their synthetic counterparts, particularly in terms of safety, efficacy, and formulation simplicity. The potential applications of these bioinspired nanomaterials extend beyond wound healing and dental infection management, heralding a promising frontier in oral health restoration. The diversified range of these nanomaterials, from Propolis, Miswak, and Chitosan nanoparticles (NPs) to pomegranate extract and <em>Matricaria chamomilla L.</em> extract-based mouthwashes, introduces an exciting new dimension to oral care.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100219"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142418210","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Delivery of N-heterocyclic drugs, acids, phenols, and thiols via Tailor−made Self−immolative linkers","authors":"Vahid Barati ,&nbsp;Anna Hruzíková ,&nbsp;Eliška Procházková ,&nbsp;Martin Zavřel ,&nbsp;Jaroslav Kozák ,&nbsp;Jana Trylčová ,&nbsp;Dominik Rejman ,&nbsp;Jan Weber ,&nbsp;Kateřina Bogdanová ,&nbsp;Milan Kolář ,&nbsp;Ondřej Baszczyňski","doi":"10.1016/j.ejmcr.2024.100216","DOIUrl":"10.1016/j.ejmcr.2024.100216","url":null,"abstract":"<div><div>Heterocyclic drugs display diverse pharmacological activities and metabolic stability. However, their poor solubility and pharmacokinetic properties often compromise bioavailability and clinical outcomes. Nevertheless, the prodrug approach provides a viable strategy to overcome unwanted attributes of drug candidates. In this proof-of-concept study, we report the synthesis and biological evaluation of glycol methylene-bridged phosphate (GMBP) prodrugs developed for heterocyclic drug delivery. Through methylene bridging, the heterocyclic nitrogen was directly attached to the phosphate, whereas the glycol moiety enabled drug release via cyclization, as confirmed by ³¹P NMR spectroscopy. Additional prodrugs of carboxylic acids, phenols, and thiols confirmed the broad application scope of our GMPB approach. Heterocyclic GMBP prodrugs were stable in aqueous buffers and activated by phospholipase CAL-B <em>in vitro</em>. Select prodrugs, including zidovudine prodrug <strong>33</strong>, were even more potent (3 nM on HIV-1) than the parent compound. These findings demonstrate that our GMBP approach is not only feasible but also highly versatile.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100216"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142418790","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Nanohybrid cerasomes: Advancements in targeted drug and gene delivery","authors":"Kalyani Pathak ,&nbsp;Mohammad Zaki Ahmad ,&nbsp;Riya Saikia ,&nbsp;Partha Protim Borthakur ,&nbsp;Pallab Pramanik ,&nbsp;Md Ariful Islam ,&nbsp;Aparoop Das ,&nbsp;Basel A. Abdel-Wahab ,&nbsp;Dibyajyoti Das ,&nbsp;Saptasikha Gogoi","doi":"10.1016/j.ejmcr.2024.100178","DOIUrl":"https://doi.org/10.1016/j.ejmcr.2024.100178","url":null,"abstract":"<div><p>Nanohybrid cerasomes represent a significant advancement in the field of drug delivery systems, offering a superior alternative to traditional cerasomes and liposomes. Cerasomes are biocompatible colloidal nanoparticles characterized by an additional polyorganosiloxane network layer that enhances their stability compared to conventional liposomes. The novel hybrid liposomal cerasome, featuring a partial ceramic or silica coating, has garnered substantial interest due to its unique structure. This structure provides better morphological stability than traditional liposomes and, in comparison to silica nanoparticles, significantly reduces overall stiffness and density. By incorporating liposomal architecture, cerasomes achieve greater biocompatibility than silica nanoparticles. This unique combination leverages the benefits of both liposomes and silica nanoparticles while mitigating their respective drawbacks, positioning cerasomes as an optimal drug delivery system. Nanohybrid cerasomes offer extended circulation residence time, enabling more efficient drug delivery to disease sites and facilitating the targeting of specific disease cells. Their potential as intracellular delivery vehicles for proteins, peptides, antisense compounds, ribozymes, and DNA is particularly noteworthy. The presence of a liposomal bilayer structure in cerasomes reduces rigidity and density, enhancing their stability and effectiveness as drug and gene delivery vehicles. This article reviews the techniques for preparing cerasomes and explores their applications in targeted drug and gene delivery systems, highlighting their advantages over conventional liposomes and silica nanoparticles.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100178"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000505/pdfft?md5=852ad277ccffe286064af8d1d12f3201&pid=1-s2.0-S2772417424000505-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141323910","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Discovery and efficacy study of an ALK inhibitor AMX6001 in anaplastic large cell lymphoma Karpas299 mice models","authors":"Debasis Das,&nbsp;Lingzhi Xie,&nbsp;Dandan Qiao,&nbsp;Yuxi Cao,&nbsp;Jianhe Jia,&nbsp;Yong Li,&nbsp;Jian Hong","doi":"10.1016/j.ejmcr.2024.100209","DOIUrl":"10.1016/j.ejmcr.2024.100209","url":null,"abstract":"<div><p>Anaplastic lymphoma kinase (ALK) is an attractive therapeutic target for the treatment of anaplastic large cell lymphoma (ALCL). We identified novel deuterated 2,4-diarylamino pyrimidine compounds as potent ALK inhibitors. The compound <strong>9</strong> (<strong>AMX6001</strong>) showed better <em>in vitro</em> activity against ALK and NPM-ALK kinase and significantly inhibited proliferation of Karpas299 and SU-DHL-1 cell lines. <em>In vivo</em> efficacy of compound <strong>9</strong> was better than reference standard ceritinib in ALCL Karpas299 mice models. Daily oral treatment of compound <strong>9</strong> (25 mg/kg) induced tumor suppression TGI up to 95.8 % in ALCL models.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100209"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000815/pdfft?md5=a3a86c8978cc4e8877ca8b225053a789&pid=1-s2.0-S2772417424000815-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142151803","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Metronidazole delivery strategies: Optimizing cancer therapy through novel approaches for enhanced delivery, cytotoxicity, and side effect reduction","authors":"Hamed Ahmadi ,&nbsp;Mohammadali Heydari ,&nbsp;Majid Abdouss ,&nbsp;Zahra Jamalpoor ,&nbsp;Sonia Fathi-karkan ,&nbsp;Abbas Rahdar ,&nbsp;Sadanand Pandey","doi":"10.1016/j.ejmcr.2024.100202","DOIUrl":"10.1016/j.ejmcr.2024.100202","url":null,"abstract":"<div><p>Metronidazole (MTZ) is a vital antimicrobial agent widely used in the treatment of various infections. However, its limited bioavailability and associated side effects necessitate the development of efficient drug delivery systems to enhance therapeutic efficacy and minimize adverse reactions. The field of nanotechnology and nanomaterials presents promising solutions for delivering MTZ, leveraging their unique properties to overcome these challenges. This comprehensive review explores a variety of nanomaterial-based approaches for MTZ delivery, emphasizing the benefits such as improved drug stability, targeted release, and enhanced bioavailability. Various nanocarrier systems, including polymeric nanoparticles, lipid-based nanocarriers, and inorganic nanoparticles, are evaluated for their potential in MTZ delivery applications. The review underscores strategies aimed at reducing MTZ's side effects through controlled release and targeted delivery, with nanocarriers facilitating sustained drug release to minimize fluctuations in drug concentrations and potentially mitigate adverse reactions linked to MTZ administration. Furthermore, innovative combination therapies involving MTZ and other drugs are investigated for their ability to enhance therapeutic outcomes and combat drug resistance. Co-delivery systems show promise in synergistically targeting infections while reducing overall dosage and associated side effects. By summarizing the latest advancements in MTZ delivery, this review provides valuable insights into the potential of nanotechnology-based strategies for optimizing MTZ therapy. These approaches have the potential to transform drug delivery, offering safer and more effective treatments for infectious diseases, and improving patient outcomes by reducing adverse effects.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100202"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000748/pdfft?md5=586d935768f5faa545b5a83aa0ad54ca&pid=1-s2.0-S2772417424000748-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142001979","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Comprehensive review of DNA gyrase as enzymatic target for drug discovery and development","authors":"K. Rajakumari ,&nbsp;K. Aravind ,&nbsp;M. Balamugundhan ,&nbsp;Manjunathan Jagadeesan ,&nbsp;Ambiga Somasundaram ,&nbsp;Parthiban Brindha Devi ,&nbsp;Pasiyappazham Ramasamy","doi":"10.1016/j.ejmcr.2024.100233","DOIUrl":"10.1016/j.ejmcr.2024.100233","url":null,"abstract":"<div><div>DNA gyrase is a member of the DNA topoisomerase protein family that catalyzes the conversion of different topological forms of DNA into one another. It is the sole enzyme that causes DNA to negatively supercoil. The enzyme is tetrameric with two GyrA (“A\") and two GyrB (“B\") subunits. DNA gyrase is an ideal target for medication because of its basic properties in bacterial cells and the lack of gyrase activity in eukaryotes. Antibacterial medications, including quinolones and derivatives based on coumarins that specifically target DNA gyrase, underscore the significance of the enzyme in the fight against bacterial infections. In addition to the typical antibiotic-binding sites, including novobiocin and fluoroquinolones, several other areas are being used in drug discovery. Simocyclinone, thiophene, gepotidacin, halogen atoms in the para position of the phenyl right-hand side (RHS) moiety, and coupled cell division B (CcdB) are examples of novel bacterial type II topoisomerase inhibitors (NBTIs). These binding sites are structurally and chemically active and inhibit the supercoiling activity of topoisomerase. This article provides an overview of DNA gyrase inhibition using synthetic and natural precursors aimed at medication development and discovery.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"12 ","pages":"Article 100233"},"PeriodicalIF":0.0,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142532743","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}