☆ 4.5 Article

Synthesis and biological evaluation of novel oxindole derivatives for imaging neurofibrillary tangles in Alzheimer's disease

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2012)

获取全文
添加到收藏夹

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 17, 页码 5700-5703

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.06.086

关键词

Oxindole; Neurofibirillary tangles; Tau protein; Alzheimer's disease

类别

Chemistry, Medicinal Chemistry, Organic

资金

  1. Funding Program for Next Generation World-Leading Researchers
  2. JSPS
  3. Grants-in-Aid for Scientific Research [23390233] Funding Source: KAKEN

向作者/读者索取更多资源

Protocol

社区支持

Reagent

社区支持

This letter describes the synthesis and biological evaluation of a novel series of radioiodinated oxindole (OI) derivatives for detecting neurofibrillary tangles (NFTs) in the brains of patients with Alzheimer's disease (AD). In binding experiments in vitro, 2-oxindole (2-OI) and 3-oxindole (3-OI) derivatives showed affinity for tau aggregates. The 3-OI derivative 14 showed the highest affinity of these derivatives. In biodistribution experiments using normal mice, the OI derivatives displayed good uptake (2.4-2.5% ID/g at 2 min) and clearance from the brain with time (0.6-1.4% ID/g at 30 min). In fluorescence staining experiments using AD brain sections, 14 clearly stained NFTs. 3-OI may serve as a new molecular scaffold for developing novel NFT imaging agents. (C) 2012 Elsevier Ltd. All rights reserved.

作者

我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.5
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

Article Clinical Neurology

Cerebral microbleeds development after stroke thrombolysis: A secondary analysis of the THAWS randomized clinical trial

Kaori Miwa, Masatoshi Koga, Manabu Inoue, Sohei Yoshimura, Makoto Sasaki, Yusuke Yakushiji, Mayumi Fukuda-Doi, Yasushi Okada, Taizen Nakase, Masafumi Ihara, Yoshinari Nagakane, Shunya Takizawa, Koko Asakura, Junya Aoki, Kazumi Kimura, Haruko Yamamoto, Kazunori Toyoda

Summary: New cerebral microbleeds developed within 36 h in 11% of patients after intravenous thrombolysis, and they were significantly associated with mixed-distribution and >= 5 cerebral microbleeds.

INTERNATIONAL JOURNAL OF STROKE (2022)

添加到收藏夹
Review Clinical Neurology

Intensive blood pressure lowering with nicardipine and outcomes after intracerebral hemorrhage: An individual participant data systematic review

Kazunori Toyoda, Sohei Yoshimura, Mayumi Fukuda-Doi, Adnan Qureshi, Renee' Hebert Martin, Yuko Y. Palesch, Masafumi Ihara, Jose Suarez, Yasushi Okada, Chung Y. Hsu, Ryo Itabashi, Yongjun Wang, Hiroshi Yamagami, Thorsten Steiner, Nobuyuki Sakai, Byung-Woo Yoon, Manabu Inoue, Kazuo Minematsu, Haruko Yamamoto, Masatoshi Koga

Summary: The study showed that rapid lowering of systolic blood pressure by continuous administration of intravenous nicardipine in patients with hyperacute intracerebral hemorrhage was associated with lower risks of hematoma expansion and 90-day death or disability, without increasing serious adverse events.

INTERNATIONAL JOURNAL OF STROKE (2022)

添加到收藏夹
Editorial Material Cardiac & Cardiovascular Systems

Endothelial BACE1: Bridging the Gap Between Hypertension and Alzheimer's Disease

Masafumi Ihara

CIRCULATION RESEARCH (2022)

添加到收藏夹
News Item Clinical Neurology

Transcriptomic mapping of the human cerebrovasculature

Masafumi Ihara, Yumi Yamamoto

Summary: Single-cell transcriptomic analyses of human brain microvessels have identified transcriptomic signatures and transcriptional changes in the cerebrovasculature in neurodegenerative diseases, which could significantly contribute to our understanding of brain health and disease.

NATURE REVIEWS NEUROLOGY (2022)

添加到收藏夹
Article Clinical Neurology

Internal Carotid Artery Tortuosity: Impact on Mechanical Thrombectomy

Junpei Koge, Kanta Tanaka, Takeshi Yoshimoto, Masayuki Shiozawa, Yuji Kushi, Tsuyoshi Ohta, Tetsu Satow, Hiroharu Kataoka, Masafumi Ihara, Masatoshi Koga, Noriko Isobe, Kazunori Toyoda

Summary: Tortuosity of the internal carotid artery (ICA) affects the outcomes of mechanical thrombectomy, with lower first pass effect rate and higher risk of intracranial hemorrhage in patients with greater tortuosity.

STROKE (2022)

添加到收藏夹
Article Clinical Neurology

Temporal Trajectory of Systolic Blood Pressure and Outcomes in Acute Intracerebral Hemorrhage: ATACH-2 Trial Cohort

Kanta Tanaka, Masatoshi Koga, Mayumi Fukuda-Doi, Adnan Qureshi, Haruko Yamamoto, Kaori Miwa, Masafumi Ihara, Kazunori Toyoda

Summary: This study used group-based trajectory modeling to analyze blood pressure changes in patients with acute intracerebral hemorrhage receiving antihypertensive treatment, and found that different blood pressure trajectories were associated with different outcomes. Specifically, the high-to-low SBP group showed increased risks of death or disability and acute kidney injury.

STROKE (2022)

添加到收藏夹
Article Clinical Neurology

Impact of Previous Stroke on Clinical Outcome in Elderly Patients With Nonvalvular Atrial Fibrillation: ANAFIE Registry

Takeshi Yoshimoto, Kazunori Toyoda, Masafumi Ihara, Hiroshi Inoue, Takeshi Yamashita, Shinya Suzuki, Masaharu Akao, Hirotsugu Atarashi, Takanori Ikeda, Ken Okumura, Yukihiro Koretsune, Wataru Shimizu, Hiroyuki Tsutsui, Atsushi Hirayama, Masahiro Yasaka, Hirofumi Maruyama, Satoshi Teramukai, Tetsuya Kimura, Yoshiyuki Morishima, Atsushi Takita, Takenori Yamaguchi

Summary: The history of stroke/TIA in elderly patients increases the risk of stroke, bleeding, and death. Among patients with prior ischemic stroke/TIA, taking direct oral anticoagulants reduces the risk of bleeding events.

STROKE (2022)

添加到收藏夹
Review Clinical Neurology

Update on the Epidemiology, Pathogenesis, and Biomarkers of Cerebral Autosomal Dominant Arteriopathy With Subcortical Infarcts and Leukoencephalopathy

Yumi Yamamoto, Yi-Chu Liao, Yi-Chung Lee, Masafumi Ihara, Jay Chol Choi

Summary: CADASIL is the most common monogenic disorder of the cerebral small blood vessels, caused by mutations in the NOTCH3 gene. Recent large-scale genomic studies have revealed a high prevalence of pathogenic NOTCH3 variants among the general population, with the highest risk being among Asians. The exact pathogenesis of CADASIL remains unclear, despite various laboratory and clinical observations being made.

JOURNAL OF CLINICAL NEUROLOGY (2023)

添加到收藏夹
Article Nutrition & Dietetics

Novel Therapeutic Potentials of Taxifolin for Obesity-Induced Hepatic Steatosis, Fibrogenesis, and Tumorigenesis

Takayuki Inoue, Bin Fu, Miwako Nishio, Miyako Tanaka, Hisashi Kato, Masashi Tanaka, Michiko Itoh, Hajime Yamakage, Kozue Ochi, Ayaka Ito, Yukihiro Shiraki, Satoshi Saito, Masafumi Ihara, Hideo Nishimura, Atsuhiko Kawamoto, Shian Inoue, Kumiko Saeki, Atsushi Enomoto, Takayoshi Suganami, Noriko Satoh-Asahara

Summary: The molecular pathogenesis of nonalcoholic steatohepatitis (NASH) involves metabolic stress and inflammatory stimuli. In this study, we found that Taxifolin treatment effectively prevented hepatic steatosis, chronic inflammation, and liver fibrosis in a NASH murine model. Taxifolin inhibited lipid accumulation in hepatocytes and increased brown adipose tissue activity. Furthermore, Taxifolin treatment after NASH development could prevent the development of liver tumors. These findings indicate the pleiotropic effects of Taxifolin for NASH treatment.

NUTRIENTS (2023)

添加到收藏夹
Editorial Material Biochemistry & Molecular Biology

Uncovering the genetic architecture of paediatric moyamoya angiopathy: implications for disease pathogenesis

Hiroyuki Ishiyama, Masafumi Ihara

EUROPEAN JOURNAL OF HUMAN GENETICS (2023)

添加到收藏夹
Article Nutrition & Dietetics

Taxifolin Suppresses Inflammatory Responses of High-Glucose-Stimulated Mouse Microglia by Attenuating the TXNIP-NLRP3 Axis

Masayo Iwasa, Hisashi Kato, Kaori Iwashita, Hajime Yamakage, Sayaka Kato, Satoshi Saito, Masafumi Ihara, Hideo Nishimura, Atsuhiko Kawamoto, Takayoshi Suganami, Masashi Tanaka, Noriko Satoh-Asahara

Summary: This study found that a high-glucose environment can increase intracellular reactive oxygen species (ROS) levels and trigger inflammation in microglial cells, leading to cognitive impairment in diabetes. However, taxifolin, a natural flavonoid, has been shown to reduce ROS levels and inhibit the activation of the TXNIP-NLRP3 axis, thereby suppressing inflammation and preventing cognitive impairment in diabetes.

NUTRIENTS (2023)

添加到收藏夹
Letter Clinical Neurology

Preservation of Dopamine Transporters in a Patient With Micrographia Due to Cerebral Infarction: A Case Report

Yoshito Arakaki, Takeshi Yoshimoto, Hiroyuki Ishiyama, Tomotaka Tanaka, Yorito Hattori, Masafumi Ihara

JOURNAL OF MOVEMENT DISORDERS (2023)

添加到收藏夹
Article Health Care Sciences & Services

Detection of Atrial Fibrillation Using Insertable Cardiac Monitors in Patients With Cryptogenic Stroke in Japan (the LOOK Study) Protocol for a Prospective Multicenter Observational Study

Satoshi Suda, Takehiro Katano, Kazuo Kitagawa, Yasuyuki Iguchi, Shigeru Fujimoto, Kenjiro Ono, Osamu Kano, Hidehiro Takekawa, Masatoshi Koga, Masafumi Ihara, Masafumi Morimoto, Hiroshi Yamagami, Tadashi Terasaki, Keiji Yamaguchi, Seiji Okubo, Yuji Ueno, Nobuyuki Ohara, Yuki Kamiya, Masataka Takeuchi, Yukako Yazawa, Yuka Terasawa, Ryosuke Doijiri, Yoshifumi Tsuboi, Kazutaka Sonoda, Koichi Nomura, Takashi Shimoyama, Akihito Kutsuna, Kazumi Kimura

Summary: This study aims to evaluate the proportion, timing, and characteristics of atrial fibrillation (AF) detection in patients with cryptogenic stroke (CS) using insertable cardiac monitors (ICMs). It also aims to compare patient characteristics and outcomes between those with AF and those without AF. The study has started and the main results are expected to be published in 2023. The findings of this study will contribute to the identification of AF markers and the development of a new and improved screening algorithm for AF detection, as well as aiding in the selection of patients for ICM implantation and the development of diagnostic criteria for CS in Japan.

JMIR RESEARCH PROTOCOLS (2023)

添加到收藏夹
Article Clinical Neurology

Seizure-associated takotsubo cardiomyopathy with Alzheimer's disease: A case report

Takehito Kuroda, Tomotaka Tanaka, Soichiro Abe, Manabu Inoue, Yoshiaki Morita, Takuto Mukaida, Takamasa Iwai, Masafumi Ihara

EPILEPTIC DISORDERS (2023)

添加到收藏夹
Article Medicine, General & Internal

Randomised placebo-controlled multicentre trial to evaluate the efficacy and safety of JTR-161, allogeneic human dental pulp stem cells, in patients with Acute Ischaemic stRoke (J-REPAIR)

Satoshi Suda, Chikako Nito, Masafumi Ihara, Yasuyuki Iguchi, Takao Urabe, Yuji Matsumaru, Nobuyuki Sakai, Kazumi Kimura

Summary: This study aims to evaluate the safety and efficacy of a novel cell-based therapy product called JTR-161 for patients with acute ischemic stroke. The study will be conducted in Japan and will use a randomized, double-blind, placebo-controlled design. The results of the study will be disseminated through informed consent forms and peer-reviewed publication.

BMJ OPEN (2022)

添加到收藏夹
Article Chemistry, Medicinal

Design and synthesis of a library of C2-substituted sulfamidoadenosines to probe bacterial permeability

Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan

Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2024)

添加到收藏夹
Article Chemistry, Medicinal

Design of MERS-CoV entry inhibitory short peptides based on helix-stabilizing strategies

Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang

Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2024)

添加到收藏夹
Article Chemistry, Medicinal

Development of novel β2-adrenergic receptor agonists for the stimulation of glucose uptake - The importance of chirality and ring size of cyclic amines

Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman

Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2024)

添加到收藏夹
Article Chemistry, Medicinal

Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2)

Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li

Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2024)

添加到收藏夹
Article Chemistry, Medicinal

The potential of Rhein's aromatic amines for Parkinson's disease prevention and treatment: α-Synuclein aggregation inhibition and disaggregation of preformed fibers

Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang

Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2024)

添加到收藏夹
Article Chemistry, Medicinal

Design, synthesis and biological evaluation of novel cationic liposomes loaded with melphalan for the treatment of cancer

Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla

Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2024)

添加到收藏夹
研讨会 海报 问题 讨论圈 基金 期刊 论文 科研社交 资讯集成 审稿人 关于我们 常见问题 移动App 隐私条款 使用条款
© Peeref 2019-2024. All rights reserved.