Bioorganic & Medicinal Chemistry Letters最新文献_第7页

N-alkyl substituted armeniaspirol analogs show potent antibiotic activity and have low susceptibility to resistance n -烷基取代的亚美尼亚吡醇类似物显示出有效的抗生素活性，并具有较低的耐药性。

IF 2.5 4区医学

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-21 DOI: 10.1016/j.bmcl.2025.130137

Michael G. Darnowski, Taylor D. Lanosky, Antonio D. Spada, Jason Ma, André R. Paquette, Christopher N. Boddy

引用次数: 0

Sensitive and reliable gastric ulcer related MicroRNA detection by bridge catalytic hairpin assembly (bCHA) mediated primer exchange reaction 桥催化发夹组装（bCHA）介导的引物交换反应灵敏可靠地检测胃溃疡相关MicroRNA。

IF 2.5 4区医学

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-21 DOI: 10.1016/j.bmcl.2025.130153

Ligong Wang , Shan Zhao , Pang Hui , Kaige Zhang

{"title":"Sensitive and reliable gastric ulcer related MicroRNA detection by bridge catalytic hairpin assembly (bCHA) mediated primer exchange reaction","authors":"Ligong Wang , Shan Zhao , Pang Hui , Kaige Zhang","doi":"10.1016/j.bmcl.2025.130153","DOIUrl":"10.1016/j.bmcl.2025.130153","url":null,"abstract":"<div><div>MicroRNAs (miRNA) have a significant role in the progression of gastric ulcer, and the sensitive and reliable detection of miRNAs is pivotal for the early diagnosis and treatment of gastrointestinal diseases. In this study, we developed a novel and efficient method for detecting miRNA-122, a crucial biomarker used to assess the prognosis of gastric ulcers. This method combines the bridge catalytic hairpin assembly (bCHA)-based target sequence recycling with the primer exchange reaction (PER), resulting in a highly sensitive and label-free approach. Specifically, the bridge CHA technique, which offers superior target recognition accuracy and increased signal amplification efficiency compared to the classic CHA procedure, can selectively identify the target miRNA and release the complementary sequence to serve as a primer to facilitate the PER. This PER process produces a large number of G-quadruplex sequences, which then bind with thioflavin T to significantly increase its fluorescence. This enhanced fluorescence is used to detect miRNA-122, with a detection limit as low as 3.12 fM. The proposed approach can achieve exact discrimination of the target miRNA-122. Due to its label-free character, high selectivity, and sensitivity, this technology can serve as a practical and universal approach for detecting different biomarkers in the early stages of gastrointestinal diseases.</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":"121 ","pages":"Article 130153"},"PeriodicalIF":2.5,"publicationDate":"2025-02-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143481895","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A review-plant medicine and its extraction components inhibit influenza virus 植物药及其提取成分抑制流感病毒的研究进展。

IF 2.5 4区医学

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-21 DOI: 10.1016/j.bmcl.2025.130151

Jiejie Lu , Zhenzhen Liu , Ziyan Li , Jiahui Su , Haojie Zhen , Ying Qu , Piet Herdewijn , Hongmin Liu , Ying Liu , Zhenya Wang

{"title":"A review-plant medicine and its extraction components inhibit influenza virus","authors":"Jiejie Lu , Zhenzhen Liu , Ziyan Li , Jiahui Su , Haojie Zhen , Ying Qu , Piet Herdewijn , Hongmin Liu , Ying Liu , Zhenya Wang","doi":"10.1016/j.bmcl.2025.130151","DOIUrl":"10.1016/j.bmcl.2025.130151","url":null,"abstract":"<div><div>Influenza is a highly prevalent and highly contagious lung disease caused by influenza viruses. The main anti-influenza strategies are vaccination and antiviral drugs. Vaccination is an effective means of prevention, but the time lag in research and development makes it difficult to respond immediately to an outbreak. Approved drugs are mainly inhibitors of neuraminidase and M2 ion channels, but, due to the variability of influenza viruses, resistance to these drugs may emerge. Botanicals and their extracts have shown unique advantages in influenza treatment and are widely used in clinics across China. However, there are few reviews on the prevention and treatment of influenza with herbal medicines. We undertook a review of relevant literature in recent years to analyze the research progress of various botanicals and their extracts in the prevention and treatment of influenza. Our review provides theoretical support for the prevention and treatment of influenza by plant-based medicines, as well as new ideas for the development of novel low-toxicity and multi-target drugs.</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":"120 ","pages":"Article 130151"},"PeriodicalIF":2.5,"publicationDate":"2025-02-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143481890","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Oligonucleotide-based telomerase inhibitors with a photoresponsive α-chloroaldehyde 具有光反应性α-氯醛的端粒酶寡核苷酸抑制剂。

IF 2.5 4区医学

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-20 DOI: 10.1016/j.bmcl.2025.130138

Kentaro Kobata, Kazuki Matsubara, Risa Nishikawa, Yuki Narita, Kazuya Matsuo, Tomonori Waku, Akio Kobori

{"title":"Oligonucleotide-based telomerase inhibitors with a photoresponsive α-chloroaldehyde","authors":"Kentaro Kobata, Kazuki Matsubara, Risa Nishikawa, Yuki Narita, Kazuya Matsuo, Tomonori Waku, Akio Kobori","doi":"10.1016/j.bmcl.2025.130138","DOIUrl":"10.1016/j.bmcl.2025.130138","url":null,"abstract":"<div><div>Telomerase, a ribonucleoprotein, is a reverse transcriptase that uses telomerase RNA component (hTR) as a template to elongate telomeric DNA at the ends of chromosomes. This enzyme plays a critical role in oncogenic cellular transformation. Therefore, the telomerase is considered an attractive target for cancer therapy. In this study, we synthesized photo-cross-linking oligodeoxyribonucleotides (ODNs) with a photoresponsive α-chloroaldehyde (PCA) moiety at the 3′-end or the 5′-end of the ODNs and evaluated the inhibition efficiencies for telomerase activity. PCA-modified ODNs with a sequence complementary to the template RNA of telomerase inhibited telomerase activity upon UV irradiation, whereas those with scramble sequence showed no significant inhibition. The 50 % inhibitory concentration (IC<sub>50</sub>) of PCA-modified ODN was significantly reduced by UV irradiation. These results indicate that PCA-modified ODN inhibits telomerase activity in a sequence-selective manner and that the inhibitory activity is enhanced by the cross-linking reaction following UV irradiation.</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":"120 ","pages":"Article 130138"},"PeriodicalIF":2.5,"publicationDate":"2025-02-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143475870","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Studies on in vitro modulatory effects to base excision repair enzymes induced by small molecule binding to Deaminated CAG repeat hairpin 研究小分子与脱氨基 CAG 重复发夹结合对碱基切除修复酶的体外调节作用。

IF 2.5 4区医学

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-19 DOI: 10.1016/j.bmcl.2025.130152

Anisa Ulhusna , Asako Murata , Kazuhiko Nakatani

引用次数: 0

Oxime functionalized Chalcones: Unveiling a new class of Chalcones with potent Antiplasmodial activity against blood-stages of Plasmodium falciparum in culture 肟功能化查尔酮：揭示一类新的查尔酮对培养的恶性疟原虫血液阶段具有有效的抗疟原虫活性。

IF 2.5 4区医学

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-18 DOI: 10.1016/j.bmcl.2025.130143

Reeta Chaudhary , Ayushee , Vinoth Rajendran , T.M. Rangarajan

{"title":"Oxime functionalized Chalcones: Unveiling a new class of Chalcones with potent Antiplasmodial activity against blood-stages of Plasmodium falciparum in culture","authors":"Reeta Chaudhary , Ayushee , Vinoth Rajendran , T.M. Rangarajan","doi":"10.1016/j.bmcl.2025.130143","DOIUrl":"10.1016/j.bmcl.2025.130143","url":null,"abstract":"<div><div>The <em>Plasmodium falciparum</em> parasite, which is responsible for malaria, has developed resistance to several first-line antimalarial drugs. To address this issue, researchers have been developing novel hybrid molecules that can inhibit parasite growth. In this study, a total of 38 chalcone oxime ethers, consisting of four different types, were evaluated for <em>in vitro</em> blood-stage antiplasmodial activity against <em>P. falciparum</em> (3D7) using SYBR green I assay. The four classes of oxime ethers showed promising to moderate antiplasmodial activity. At least one molecule from each class was potent, with the IC<sub>50</sub> values of less than 5 μg/mL. Among the four classes, chalcone-chalconeoxime ethers (CCOE) were the most effective, with the IC<sub>50</sub> values of 1.55 μg/mL and 1.4 μg/mL for <strong>CCOE-2</strong> and <strong>CCOE-5</strong>, respectively. The most potent molecules, <strong>CKOE-13</strong>, <strong>COAE-2</strong>, <strong>CCOE-2</strong>, and <strong>CCOE-5</strong>, were tested against the chloroquine-resistant strain <em>P. falciparum</em> (INDO) exhibited IC<sub>50</sub> values of less than 5 μg/mL. Notably, the most potent molecules did not induce hemolysis at concentrations up to 50 μg/mL. These findings highlight a new class of chalconeoxime ethers as potent antiplasmodial agents, warranting further exploration of their biological activities.</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":"121 ","pages":"Article 130143"},"PeriodicalIF":2.5,"publicationDate":"2025-02-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143466586","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Dual-acting β-Aminothiochromones: Design, synthesis, and evaluation as antimicrobial and anti-angiogenic agents 双作用β-氨基硫代色素：抗菌和抗血管生成药物的设计、合成和评价。

IF 2.5 4区医学

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-17 DOI: 10.1016/j.bmcl.2025.130140

M.S. Ajay Krishna , K.T. Ashitha , Meghashyama Prabhakara Bhat , Muthuraj Rudrappa , K.S. Sandhya , N.C. Lima , D. Basavaraja , Sunil Varughese , Sreenivasa Nayaka , Sasidhar B. Somappa

{"title":"Dual-acting β-Aminothiochromones: Design, synthesis, and evaluation as antimicrobial and anti-angiogenic agents","authors":"M.S. Ajay Krishna , K.T. Ashitha , Meghashyama Prabhakara Bhat , Muthuraj Rudrappa , K.S. Sandhya , N.C. Lima , D. Basavaraja , Sunil Varughese , Sreenivasa Nayaka , Sasidhar B. Somappa","doi":"10.1016/j.bmcl.2025.130140","DOIUrl":"10.1016/j.bmcl.2025.130140","url":null,"abstract":"<div><div>The quest for novel antimicrobials is critical due to emerging resistance by new microorganism strains. In these circumstances, we designed and synthesized a series of β-aminothiochromones by employing an aziridines ring-opening strategy to discover antimicrobial agents that are effective against multidrug-resistant (MDR) bacteria. Structures of the compounds [<strong>3(a-m)</strong> and <strong>3a(a-o)</strong>] were well characterized and confirmed by the spectroscopic, analytical and single crystal X-ray analysis. Further, we conducted the in vitro antimicrobial assessment studies against selected Gram-positive, and Gram-negative bacterial strains and two fungal strains. In preliminary screening, all synthesized compounds exhibited moderate activity compared to tested standard drugs Ampicillin, Ciprofloxacin and Fluconazole wherein, <strong>3</strong> <strong>m</strong> and <strong>3ae</strong> displayed higher anti-microbial activities. In addition, these analogues exhibited anti-angiogenic properties on HepG2 cells. The in-silico studies on promising hits, <strong>3</strong> <strong>m</strong> and <strong>3ae</strong> on proteins DNA gyrase and Topoisomerase IV indicate that these hybrids possess better binding energy in comparison with standard drugs. Thus, based on in vitro and silico studies, the newly synthesized compounds appear to be potential scaffolds for antimicrobial and anti-angiogenic drug discovery initiatives.</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":"120 ","pages":"Article 130140"},"PeriodicalIF":2.5,"publicationDate":"2025-02-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143456544","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Discovery of novel WRN inhibitors for treating MSI-H colorectal cancers 发现治疗MSI-H结直肠癌的新型WRN抑制剂。

IF 2.5 4区医学

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-15 DOI: 10.1016/j.bmcl.2025.130141

Byul Moon , Ahra Go , Seulki Park , Hyun Jin Kim , Dongju An , Jaehoon Kim , Joo-Youn Lee , Jeong-Hoon Kim , Jong Yeon Hwang , Jung-Ae Kim

引用次数: 0

Design, synthesis and biological evaluation of Streptazolin analogs as anti-inflammatory agents 链他唑啉类似物抗炎作用的设计、合成及生物学评价

IF 2.5 4区医学

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-14 DOI: 10.1016/j.bmcl.2025.130139

Shan Lu , Zhuang Li , Peng Jiang , Bo Jiang , Shanqin Huang , Xinhang Su , Ke Ma , Ying Xu , Lingling Ding , Di Mao

引用次数: 0

Radiosynthesis and in vivo evaluation of [18F]BEAN as a potential mitochondria-based PET biomarker for metabolic disorders [18F]BEAN作为代谢紊乱的潜在线粒体PET生物标志物的放射合成和体内评价。

IF 2.5 4区医学

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-02-14 DOI: 10.1016/j.bmcl.2025.130142

Charalambos Kaittanis , Hyunjung Kim , Tyler Teceno , Yoann Petibon , Ashley Knight , Matthew Crouthamel , Anthony P. Belanger , Zhaoming Xiong , Wanida Ruangsiriluk , Meera Modi , Rizwana Islam , Madhu Natarajan , Nikolaos Papaioannou , Christopher T. Winkelmann , Johannes Tauscher , Paul McQuade

{"title":"Radiosynthesis and in vivo evaluation of [18F]BEAN as a potential mitochondria-based PET biomarker for metabolic disorders","authors":"Charalambos Kaittanis , Hyunjung Kim , Tyler Teceno , Yoann Petibon , Ashley Knight , Matthew Crouthamel , Anthony P. Belanger , Zhaoming Xiong , Wanida Ruangsiriluk , Meera Modi , Rizwana Islam , Madhu Natarajan , Nikolaos Papaioannou , Christopher T. Winkelmann , Johannes Tauscher , Paul McQuade","doi":"10.1016/j.bmcl.2025.130142","DOIUrl":"10.1016/j.bmcl.2025.130142","url":null,"abstract":"<div><div>Changes in metabolism are associated with several prevalent and rare diseases, like Hunter syndrome (MPS II). These alterations result in changes in mitochondrial function, therefore having non-invasive imaging biomarkers to detect this pathophysiological hallmark is a key objective of translational medicine. Here we report the synthesis and <em>in vivo</em> evaluation of the [<sup>18</sup>F]berberine analogue ([<sup>18</sup>F]BEAN), in both wildtype animals and a mouse model of Hunter's disease. PET/CT imaging revealed that [<sup>18</sup>F]BEAN could detect mitochondrial dysfunction in the heart, liver, and brain of Hunter's disease (Ids KO) mice. These data suggest that [<sup>18</sup>F]BEAN may be a viable translational PET biomarker for the imaging of diverse pathologies that have impaired mitochondrial function.</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":"120 ","pages":"Article 130142"},"PeriodicalIF":2.5,"publicationDate":"2025-02-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143432078","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0