39679-61-3Relevant academic research and scientific papers
Certain 4-iminoflavones derivatives: Synthesis, docking studies, antiasthmatic and antimicrobial agents
Khah, Shaila,Goyal, Rohit,Chabba, Ankush,Jaiswal, Varun,Sharma, Gaurav,Naushad
, p. 1687 - 1696 (2016/07/06)
In this present study, certain substituted 4-iminoflavone derivatives 5(a-j) were synthesized. All the synthesized compounds were evaluated for antiasthmatic and antimicrobial activity. Among the synthesized compounds, 5f was found to be the most promising against asthmatic models, whilst, 5h was found active against all the microbial strains. Antiasthmatic activity was correlated and evaluated with various models, e.g., citric acid induced cough model, OVA induced asthma model (biochemical estimation for cell infiltrations, estimation of lipid peroxidation and glutathione and estimation of TNF-α and IL-6 and histamine induced response). Compound 5f was found to show 2.20 ± 0.047 number of cough whilst codeine showed 1.40 ± 0.548; compound 5f produced considerable reduction in neutrophils, lymphocytes, eosinophils and leukocytes; decrease in LPO level (lung and BALF) and increment in GSH level (lungand BALF); and decreased the level of TNF-α and IL-6, respectively. On the other hand, 5h showed MIC 6.25 μg/mL against B. subtilis and S. aureus, 3.1 μg/mL against E. coli, 1.55 μg/mL against S. typhi and 6.25 μg/mL against C. albicans, respectively. In addition to gain better understanding on the biological activities of synthesized compounds, molecular docking study was performed within the binding site of human histamine H1 receptor and Glc-6-P synthase revealing compound 5f and 5h as best fit within the respective receptor pockets.
99mTc/Re complexes based on flavone and aurone as SPECT probes for imaging cerebral β-amyloid plaques
Ono, Masahiro,Ikeoka, Ryoichi,Watanabe, Hiroyuki,Kimura, Hiroyuki,Fuchigami, Takeshi,Haratake, Mamoru,Saji, Hideo,Nakayama, Morio
supporting information; experimental part, p. 5743 - 5748 (2010/11/18)
Two 99mTc/Re complexes based on flavone and aurone were tested as potential probes for imaging β-amyloid plaques using single photon emission computed tomography. Both 99mTc-labeled derivatives showed higher affinity for Aβ(1-42) aggregates than did 99mTc-BAT. In sections of brain tissue from an animal model of AD, the Re-flavone derivative 9 and Re-aurone derivative 19 intensely stained β-amyloid plaques. In biodistribution experiments using normal mice, 99mTc-labeled flavone and aurone displayed similar radioactivity pharmacokinetics. With additional modifications to improve their brain uptake, 99mTc complexes based on the flavone or aurone scaffold may serve as probes for imaging cerebral β-amyloid plaques.
A facile synthesis of flavones catalysed by gallium(III) triflate
Jin, Can,He, Fei,Wu, Huayue,Chen, Jiuxi,Su, Weike
experimental part, p. 27 - 29 (2009/09/25)
Ga(OTf)3 was explored as a novel catalyst for the cyclisation of 1-(2-hydroxyphenyl)-3-aryl-1,3-propanediones in nitromethane to flavones with excellent yields.
18F-labeled flavones for in vivo imaging of β-amyloid plaques in Alzheimer's brains
Ono, Masahiro,Watanabe, Rumi,Kawashima, Hidekazu,Kawai, Tomoki,Watanabe, Hiroyuki,Haratake, Mamoru,Saji, Hideo,Nakayama, Morio
experimental part, p. 2069 - 2076 (2009/06/06)
In vivo imaging of β-amyloid (Aβ) aggregates in the brain may lead to early detection of Alzheimer's disease (AD) and monitoring of the progression and effectiveness of treatment. The purpose of this study was to develop novel 18F-labeled amyloid-imaging probes based on flavones as a core structure. Fluoropegylated (FPEG) flavone derivatives were designed and synthesized. The affinity of the derivatives for Aβ aggregates varied from 5 to 321 nM. In brain sections of AD model mice, FPEG flavones with the dimethylamino group intensely stained β-amyloid plaques. In biodistrubution experiments using normal mice, they displayed high uptake in the brain ranging from 2.9 to 4.2%ID/g at 2 min postinjection. The radioactivity washed out from the brain rapidly (1.3-2.0%ID/g at 30 min), which is highly desirable for β-amyloid imaging agents. FPEG flavones may be potential PET imaging agents for β-amyloid plaques in Alzheimer's brains.
COMPOSITION FOR AMYLOID-ASSOCIATED DISEASE DIAGNOSIS
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Page/Page column 5; 35; 44; 53, (2010/11/28)
A composition for diagnosing amyloid-related diseases, which comprises a flavone derivative, a chalcone derivative, a styrylchromone derivative, or a coumarin derivative, is provided. These compounds have high binding specificity to an amyloid β protein,
An environmentally benign synthesis of flavones from 1,3-diketones using silica gel supported NaHSO4 catalyst
Kucukislamoglu, Mustafa,Nebioglu, Mehmet,Zengin, Mustafa,Arslan, Mustafa,Yayli, Nurettin
, p. 556 - 557 (2007/10/03)
A simple and enviromentaly benign method for synthesis of flavones is described via dehydrative cyclisation of o-hydroxydibenzoylmethane using silica gel supported NaHSO4 catalyst.
