Category: 1827-27-6

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Design, Synthesis, and Structure-Activity Relationship of Indole-3-glyoxylamide Libraries Possessing Highly Potent Activity in a Cell Line Model of Prion Disease, published in 2009-12-10, which mentions a compound: 1827-27-6, Name is 5-Amino-2-fluoropyridine, Molecular C5H5FN2, Safety of 5-Amino-2-fluoropyridine.

Transmissible spongiform encephalopathies (TSEs) are a family of invariably fatal neurodegenerative disorders for which no effective curative therapy currently exists. We report here the synthesis of a library of indole-3-glyoxylamides and their evaluation as potential antiprion agents. A number of compounds demonstrated submicromolar activity in a cell line model of prion disease together with a defined structure-activity relationship, permitting the design of more potent compounds that effected clearance of scrapie in the low nanomolar range. Thus, the indole-3-glyoxylamides described herein constitute ideal candidates to progress to further development as potential therapeutics for the family of human prion disorders.

There are many compounds similar to this compound(1827-27-6)Safety of 5-Amino-2-fluoropyridine. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Synthetic Route of C5H5FN2. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Synthesis of 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones via directed lithiation of 2-substituted 5-aminopyridine derivatives.

Directed lithiation of Boc or pivaloyl derivatives of 2-substituted 5-aminopyridines I (R = Cl, F, OMe, R1 = COnCMe3, X = H, n = 1, 2) with BuLi-TMEDA in di-Et ether at -10°C gave 4-lithio derivatives which were quenched with CO2 to give the analogous C-4 carboxylic acids I (X = CO2H). Hydrolysis of the protecting groups with either TFA or aqueous KOH gave 2-substituted 5-aminopyridine-4-carboxylic acids I (R1 = H, X = CO2H) which were converted to 6-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones II by reaction with formamide or, more optionally, formamidine acetate. Boc protected aminopyridines provided the best overall results, with synthesis of these derivatives best achieved by direct reaction of the aminopyridine with di-tert-Bu dicarbonate in the absence of added base.

There are many compounds similar to this compound(1827-27-6)Synthetic Route of C5H5FN2. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about HDAC4 Inhibitors with Cyclic Linker and Non-hydroxamate Zinc Binding Group: Design, Synthesis, HDAC Screening and in vitro Cytotoxicity evaluation., the main research direction is HDAC inhibitor screening cytotoxicity cyclic linker nonhydroxamate zinc binding.Category: pyrazines.

Recent evidences highlight the usefulness of small mol. (Histone deacetylase 4) HDAC4 inhibitors in the several preclin. paradigms. Major toxicity and mutagenicity issues associated with hydroxamate HDAC inhibitors, stimulated us to develop potent non-hydroxamate inhibitors. In the present work a novel series of thiazolidinedione (TZD) derivatives with pyridine as cyclic linker and TZD ring as zinc binding group was designed and screened in a panel of isoenzymes of HDACs, wherein the most potent compounds exhibiting HDAC4 IC50-values<5 μM were 5 v, 5 w, 5 y and 5 z (IC50=4.2±1 μM, 0.75±0.03 μM, 4.9±0.5 and 2.3±0.5 μM, resp.). The docking studies displayed the unique binding mode of this series of compound at active site of HDAC4, wherein TZD ring was indicated as zinc binding group. Further, 5 w and 5 y were found as the most potent antiproliferative agent in lymphoblastic leukemia (CCRF-CEM) and breast cancer MDA-MB-231 cells. Compound 5 y was found to induce the apoptosis and DNA fragmentation of CEM cells. The western blotting anal. of 5 y also showed the presence of cleaved caspases supporting their apoptotic nature. Further, Class IIa (HDAC4) selectivity of 5 y was also supported by western blotting observations, wherein 5 y caused the accumulation of acetylated H3 but not of acetylated Tubulin. Thus, our findings endorse the further investigation of this series of compounds for their potential as targeted cancer therapeutic agents. There are many compounds similar to this compound(1827-27-6)Category: pyrazines. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Quality Control of 5-Amino-2-fluoropyridine. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Development of highly sensitive fluorescent assays for fatty acid amide hydrolase. Author is Huang, Huazhang; Nishi, Kosuke; Tsai, Hsing-Ju; Hammock, Bruce D..

Fatty acid amide hydrolase (FAAH) is a pharmaceutical target whose inhibition may lead to valuable therapeutics. Sensitive substrates for high-throughput assays are crucial for the rapid-screening FAAH inhibitors. Here we describe the development of novel and highly sensitive fluorescent assays for FAAH based on substituted aminopyridines. Examining the relationship between the structure and the fluorescence of substituted aminopyridines suggested that a methoxy group in the para position relative to the amino group in aminopyridines greatly increased the fluorescence (i.e., quantum yields approach unity). These novel fluorescent reporters had a high Stokes’ shift of 94 nm, and their fluorescence in buffer systems increased with pH values from neutral to basic. Fluorescent substrates with these reporters displayed a very low fluorescent background and high aqueous solubility Most importantly, fluorescent assays for FAAH based on these substrates were at least 25 times more sensitive than assays using related compounds with published colorimetric or fluorescent reporters. This property results in shorter assay times and decreased protein concentrations in the assays. Such sensitive assays will facilitate distinguishing the relative potency of powerful inhibitors of FAAH. When these fluorescent substrates were applied to human liver microsomes, results suggested that there was at least one amide hydrolase in addition to FAAH that could hydrolyze long-chain fatty acid amides. These results show that these fluorescent substrates are very valuable tools in FAAH activity assays including screening inhibitors by high-throughput assays instead of using the costly and labor-intensive radioactive ligands. Potential applications of novel fluorescent reporters are discussed.

There are many compounds similar to this compound(1827-27-6)Quality Control of 5-Amino-2-fluoropyridine. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Computed Properties of C5H5FN2. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Design, synthesis and biological evaluation of indole-2-carboxylic acid derivatives as IDO1/TDO dual inhibitors. Author is Cui, Guonan; Lai, Fangfang; Wang, Xiaoyu; Chen, Xiaoguang; Xu, Bailing.

Indoleamine 2,3-dioxygenase 1 (IDO1) and tryptophan 2,3-dioxygenase (TDO) are involved in the key steps of tryptophan metabolism and are potential new targets for tumor immunotherapy. In this work, a variety of indole-2-carboxylic acid derivatives I (R1 = H, 7-F, NHAc, etc.; X = NH, NMe, S; Y = NH, S, -NHCH2-, etc.; Ar = 4-F-3-Cl-C6H3, 4-F-3-OMe-C6H3, 3-Cl-3-OMe-C6H3, etc.) were synthesized, and their inhibitory activities against both enzymes along with structure-activity relationships were investigated. As a result, a number of 6-acetamido-indole-2-carboxylic acid derivatives were found to be potent dual inhibitors with IC50 values at low micromolar levels. Among them, compound I (R1 = 6-NHAc, X = N, Y = NH, Ar = 3,4-di-F-C6H3) was the most potent inhibitor with an IC50 value of 1.17μM for IDO1, and 1.55μM for TDO, resp. In addition, a para-benzoquinone derivative II, resulted from the oxidation of compound I (R1 = 6-NHEt, X = NH, Y = NH, Ar = 4-F-3-Cl-C6H3), was also identified and it showed strong inhibition against the two enzymes with IC50 values at the double digit nanomolar level. Using mol. docking and mol. dynamic simulations, authors predicted the binding modes of this class of compounds within IDO1 and TDO binding pocket. The results provide insights for further structural optimization of this series of IDO1/TDO dual inhibitors.

There are many compounds similar to this compound(1827-27-6)Computed Properties of C5H5FN2. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Discovery of 2-(4-(2-fluoroethoxy)piperidin-1-yl)-9-methyl-9H-pyrrolo[2,3-b:4,5-c’]dipyridine ([18F]PI-2014) as PET tracer for the detection of pathological aggregated tau in Alzheimer’s disease and other tauopathies.Related Products of 1827-27-6.

The compound screening was initiated with a direct staining assay to identify compounds binding to Tau aggregates and not Abeta plaques using human brain sections derived from late stage Alzheimer’s disease donors. The binding of Tau aggregate selective compounds was then quant. assessed with human brain derived paired helical filaments utilizing the label-free Back Scattering Interferometry assay. In vivo biodistribution experiments of selected fluorine-18 labeled compounds were performed in mice to assess brain uptake, brain washout, and defluorination. Compound 11 emerged as the most promising candidate, displaying high in vitro binding affinity and selectivity to neurofibrillary tangles. Fluorine-18 labeled compound 11 showed high brain uptake and rapid washout from the mouse brain with no observed bone uptake. Furthermore, compound 11 was able to detect Tau aggregates in tauopathy brain sections from corticobasal degeneration, progressive supranuclear palsy, and Pick’s disease donors. Thus, 2-(4-(2-fluoroethoxy)piperidin-1-yl)-9-methyl-9H-pyrrolo[2,3-b:4,5-c’]dipyridine (PI-2014, compound 11) was selected for characterization in a first-in-human study.

There are many compounds similar to this compound(1827-27-6)Related Products of 1827-27-6. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Quality Control of 5-Amino-2-fluoropyridine. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Copper-Catalyzed Electrochemical C-H Amination of Arenes with Secondary Amines. Author is Yang, Qi-Liang; Wang, Xiang-Yang; Lu, Jia-Yan; Zhang, Li-Pu; Fang, Ping; Mei, Tian-Sheng.

Electrochem. oxidation represents an environmentally friendly solution to conventional methods that require caustic stoichiometric chem. oxidants. However, C-H functionalizations merging transition-metal catalysis and electrochem. techniques are, to date, largely confined to the use of precious metals and divided cells. Herein, the authors report the 1st examples of Cu-catalyzed electrochem. C-H aminations of arenes at room temperature using undivided electrochem. cells, thereby providing a practical solution for the construction of arylamines. The use of Bu4NI as a redox mediator is crucial for this transformation. From mechanistic studies including kinetic profiles, isotope effects, cyclic voltammetric analyses, and radical inhibition experiments, the reaction appears to proceed via a single-electron-transfer (SET) process, and a high valent Cu(III) species is likely involved. These findings provide a new avenue for transition-metal-catalyzed electrochem. C-H functionalization reactions using redox mediators.

There are many compounds similar to this compound(1827-27-6)Quality Control of 5-Amino-2-fluoropyridine. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Related Products of 1827-27-6. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Synthesis and evaluation of radiolabeled AGI-5198 analogues as candidate radiotracers for imaging mutant IDH1 expression in tumors. Author is Chitneni, Satish K.; Reitman, Zachary J.; Spicehandler, Rebecca; Gooden, David M.; Yan, Hai; Zalutsky, Michael R..

Mutations in the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) are commonly found in gliomas. AGI-5198, a potent and selective inhibitor of the mutant IDH1 enzyme, was radiolabeled with radioiodine and fluorine-18. These radiotracers were evaluated as potential probes for imaging mutant IDH1 expression in tumors with positron emission tomog. (PET). Radioiodination of AGI-5198 was achieved using a tin precursor in 79±6% yield (n=9), and 18F-labeling was accomplished by the Ugi reaction in a decay-corrected radiochem. yield of 2.6±1.6% (n=5). The inhibitory potency of the analogous nonradioactive compounds against mutant IDH1 (IDH1-R132H) was determined in enzymic assays. Cell uptake studies using radiolabeled AGI-5198 analogs revealed somewhat higher uptake in IDH1-mutated cells than that in wild-type IDH1 cells. The radiolabeled compounds displayed favorable tissue distribution characteristics in vivo, and good initial uptake in IDH1-mutated tumor xenografts; however, tumor uptake decreased with time. Radioiodinated AGI-5198 exhibited higher tumor-to-background ratios compared with 18F-labeled AGI-5198; unfortunately, similar results were observed in wild-type IDH1 tumor xenografts as well, indicating lack of selectivity for mutant IDH1 for this tracer. These results suggest that AGI-5198 analogs are not a promising platform for radiotracer development. Nonetheless, insights gained from this study may help in design and optimization of novel chem. scaffolds for developing radiotracers for imaging the mutant IDH1 enzyme.

I hope my short article helps more people learn about this compound(5-Amino-2-fluoropyridine)Related Products of 1827-27-6. Apart from the compound(1827-27-6), you can read my other articles to know other related compounds.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Name: 5-Amino-2-fluoropyridine. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Sulfonamide Synthesis via Calcium Triflimide Activation of Sulfonyl Fluorides. Author is Mukherjee, Paramita; Woroch, Cristian P.; Cleary, Leah; Rusznak, Mark; Franzese, Ryan W.; Reese, Matthew R.; Tucker, Joseph W.; Humphrey, John M.; Etuk, Sarah M.; Kwan, Sabrina C.; am Ende, Christopher W.; Ball, Nicholas D..

A method using calcium triflimide [Ca(NTf2)2] as a Lewis acid to activate sulfonyl fluorides toward nucleophilic addition with amines is described. The reaction converts a wide array of sterically and electronically diverse sulfonyl fluorides and amines into the corresponding sulfonamides in good yield.

I hope my short article helps more people learn about this compound(5-Amino-2-fluoropyridine)Name: 5-Amino-2-fluoropyridine. Apart from the compound(1827-27-6), you can read my other articles to know other related compounds.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

HPLC of Formula: 1827-27-6. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about 18F-Labeled Pyrido[3,4-d]pyrimidine as an Effective Probe for Imaging of L858R Mutant Epidermal Growth Factor Receptor. Author is Kimura, Hiroyuki; Okuda, Haruka; Ishiguro, Masumi; Arimitsu, Kenji; Makino, Akira; Nishii, Ryuichi; Miyazaki, Anna; Yagi, Yusuke; Watanabe, Hiroyuki; Kawasaki, Ikuo; Ono, Masahiro; Saji, Hideo.

In non-small-cell lung carcinoma patients, L858R mutation of epidermal growth factor receptor (EGFR) are often found and mol. target therapy using EGFR tyrosine kinase inhibitors is effective for the patients. However, the treatment frequently develops drug resistance by secondary mutation, of which approx. 50% is a T790M mutation. Thus, the ability to predict whether EGFR will undergo secondary mutation is extremely important. We synthesized a novel radiofluorinated 4-(anilino)pyrido[3,4-d]pyrimidine derivative ([18F]APP-1) and evaluated its potential as a positron emission tomog. (PET) imaging probe to discriminate different tumor of mutation. EGFR inhibition assay, cell-uptake and biodistribution study showed that [18F]APP-1 binds specifically to the L858R mutant EGFR but not to the L858R/T790M mutant. Finally, PET imaging study using [18F]APP-1 with tumor-bearing mice, the H3255 tumor (L858R mutant) was more clearly visualized than the H1975 tumor (L858R/T790M mutant).

I hope my short article helps more people learn about this compound(5-Amino-2-fluoropyridine)HPLC of Formula: 1827-27-6. Apart from the compound(1827-27-6), you can read my other articles to know other related compounds.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem