Category: 98-97-5

In 2020 ACS MED CHEM LETT published article about 2,4-METHANOPROLINE in [Duffy, James; Laleu, Benoit] Med Malaria Venture, CH-1215 Geneva 15, Switzerland; [Cox, Brian; Zdorichenko, Victor; Bellanger, Corentin; Bishop, Stephen J.] Univ Sussex, Photodivers Ltd, Sch Life Sci, Brighton BN1 9QJ, E Sussex, England; [Hurcum, Jessica] Univ Sussex, Sch Life Sci, Brighton BN1 9QJ, E Sussex, England; [Booker-Milburn, Kevin, I; Elliott, Luke D.] Univ Bristol, Sch Chem, Bristol BS8 1TS, Avon, England; [Booker-Milburn, Kevin, I; Robertson-Ralph, Michael] Univ Bristol, Sch Chem, Photodivers Ltd, Bristol BS8 1TS, Avon, England; [Swain, Christopher J.] Cambridge MedChem Consulting, Cambridge CB22 4RN, England; [Hallyburton, Irene; Anderson, Mark] Univ Dundee, Wellcome Ctr Antiinfect Res, Drug Discovery Unit, Dundee DD1 5EH, Scotland in 2020, Cited 18. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. SDS of cas: 98-97-5

We utilized synthetic photochemistry to generate novel sp 3 -rich scaffolds and report the design, synthesis, and biological testing of a diverse series of amides based on the 1-(amino-methyl)-2-benzyl-2-azabicyclo[2.1.1]hexane scaffold. Preliminary antimalarial screening of the library provided promising compounds with activity in the 1-5 mu M range with an enhanced hit rate. Further evaluation (solubility, drug metabolism and pharmacokinetics (DMPK), and toxicity) of a selected compound (9) suggested that this series represents an excellent opportunity for further optimization with the framework offering multiple opportunities for the addition of uniquely vectorally positioned extra functionality.

Welcome to talk about 98-97-5, If you have any questions, you can contact Cox, B; Duffy, J; Zdorichenko, V; Bellanger, C; Hurcum, J; Laleu, B; Booker-Milburn, KI; Elliott, LD; Robertson-Ralph, M; Swain, CJ; Bishop, SJ; Hallyburton, I; Anderson, M or send Email.. SDS of cas: 98-97-5

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

An article Factors affecting the metal-enhanced luminescence of lanthanide complexes by Ag@SiO2 nanoparticles WOS:000573230200005 published article about FLUORESCENCE; SILVER; SURFACE in [Zhao, Yanfang; Wang, Ailing; Kang, Jie; Chu, Haibin; Zhang, Haixia; Zhao, Yongliang] Inner Mongolia Univ, Coll Chem & Chem Engn, Hohhot 010021, Peoples R China; [Zhao, Yanfang] Inner Mongolia Vocat Coll Chem Engn, Hohhot 010070, Peoples R China in 2020, Cited 40. Name: Pyrazine-2-carboxylic acid. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Metal-enhanced luminescence (MEL) via Ag@SiO2 nanoparticles provides a promising strategy for the superior luminescence of lanthanide complexes. However, because of the delicate structure of the composites of Ag@SiO2 and complexes, it remains a great challenge to achieve the ideal MEL effect. Herein, five types of Ag@SiO2 nanoparticles with distinct core sizes (100 and 46 nm) and varied silica shell thickness (3, 24, 32, 52 and 55 nm) were prepared. Four kinds of lanthanide complexes RE(BA)(3)center dot H2O and RE(pyca)(3)center dot 2H(2)O (RE = Eu and Tb, BA = benzoate, pyca = 2-pyrazine carboxylate) were synthesized. A series of REL3-Ag@SiO2 (L = BA(-), pyca(-)) composite nanoparticles were prepared through the interaction of the Ag@SiO2 nanoparticles and the complexes. The adsorption of the complexes on the surface of Ag@SiO2 nanoparticles was confirmed by transmission electron microscope and energy dispersive X-ray spectroscopy. Luminescence property investigation showed that the factors affecting the MEL effect included the excitation and emission wavelength of lanthanide complexes, the kinds of lanthanide ions and organic ligands, as well as the core size and shell thickness of Ag@SiO2. Among these factors, the excitation wavelength of lanthanide complexes and the SiO2 shell thickness were found to play decisive roles. Finally, 25.92 times enhancement in luminescent intensity and 7.4 times increase in luminescence quantum yield can be achieved on Tb(BA)(3)center dot H2O by Ag@SiO2 with core size of 46 nm and shell thickness of 24 nm.

Bye, fridends, I hope you can learn more about C5H4N2O2, If you have any questions, you can browse other blog as well. See you lster.. Name: Pyrazine-2-carboxylic acid

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Category: Pyrazines. Recently I am researching about TUBERCULOSIS; RESISTANCE; MUTATIONS; PROTEASE; COMPLEX, Saw an article supported by the Singapore Ministry of Health’s National Medical Research CouncilNational Medical Research Council, Singapore [NMRC/TCR/011-NUHS/2014, NMRC/CG/013/2013]; Yong Loo Lin School of Medicine graduate scholarship; National Institute of Allergy and Infectious Diseases of the National Institutes of HealthUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute of Allergy & Infectious Diseases (NIAID) [2R01AI10639805, P01AI095208]; Bill and Melinda Gates FoundationBill & Melinda Gates Foundation [OPP1181211]; National Research Foundation (NRF) SingaporeNational Research Foundation, Singapore [NRF-CRP18-2017-01]. Published in NATURE PUBLISHING GROUP in LONDON ,Authors: Gopal, P; Sarathy, JP; Yee, M; Ragunathan, P; Shin, J; Bhushan, S; Zhu, JH; Akopian, T; Kandror, O; Lim, TK; Gengenbacher, M; Lin, QS; Rubin, EJ; Gruber, G; Dick, T. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Pyrazinamide is a sterilizing first-line tuberculosis drug. Genetic, metabolomic and biophysical analyses previously demonstrated that pyrazinoic acid, the bioactive form of the prodrug pyrazinamide (PZA), interrupts biosynthesis of coenzyme A in Mycobacterium tuberculosis by binding to aspartate decarboxylase PanD. While most drugs act by inhibiting protein function upon target binding, we find here that pyrazinoic acid is only a weak enzyme inhibitor. We show that binding of pyrazinoic acid to PanD triggers degradation of the protein by the caseinolytic protease ClpC1-ClpP. Thus, the old tuberculosis drug pyrazinamide exerts anti-bacterial activity by acting as a target degrader, a mechanism of action that has recently emerged as a successful strategy in drug discovery across disease indications. Our findings provide the basis for the rational discovery of next generation PZA.

Category: Pyrazines. Welcome to talk about 98-97-5, If you have any questions, you can contact Gopal, P; Sarathy, JP; Yee, M; Ragunathan, P; Shin, J; Bhushan, S; Zhu, JH; Akopian, T; Kandror, O; Lim, TK; Gengenbacher, M; Lin, QS; Rubin, EJ; Gruber, G; Dick, T or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

An article Design, synthesis, in vitro and in vivo evaluation against MRSA and molecular docking studies of novel pleuromutilin derivatives bearing 1, 3, 4-oxadiazole linker WOS:000661874800004 published article about RESISTANCE; ANTIBIOTICS; ANIMALS in [Liu, Jie; Zhang, Guang-Yu; Zhang, Zhe; Li, Bo; Chai, Fei; Wang, Qi; Zhou, Zi-Dan; Xu, Ling-Ling; Wang, Shou-Kai; Jin, Zhen; Tang, You-Zhi] South China Agr Univ, Coll Vet Med, Guangdong Prov Key Lab Vet Pharmaceut Dev & Safet, Guangzhou 510642, Peoples R China; [Jin, Zhen; Tang, You-Zhi] Guangdong Lab Lingnan Modern Agr, Guangzhou 510642, Peoples R China in 2021, Cited 29. COA of Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

A class of pleuromutilin derivatives containing 1, 3, 4-oxadiazole were designed and synthesized as potential antibacterial agents against Methicillin-resistant staphylococcus aureus (MRSA). The ultrasound-assisted reaction was proposed as a green chemistry method to synthesize 1, 3, 4-oxadiazole derivatives (intermediates 85-110). Among these pleuromutilin derivatives, compound 133 was found to be the strongest antibacterial derivative against MRSA (MIC = 0.125 mu g/mL). Furthermore, the result of the time-kill curves displayed that compound 133 could inhibit the growth of MRSA in vitro quickly (- 4.36 log10 CFU/mL reduction). Then, compound 133 (1.82 log10 CFU/mL) displayed superior in vivo antibacterial efficacy than tiamulin (- 0.82 log10 CFU/mL) in reducing MRSA load in mice thigh model. Besides, compound 133 exhibited low cytotoxicity to RAW 264.7 cells. Molecular docking studies revealed that compound 133 was successfully localized in the binding pocket of 50S ribosomal subunit (delta Gb = -10.50 kcal/mol). The results indicated that these pleuromutilin derivatives containing 1, 3, 4-oxadiazole might be further developed into novel antibiotics against MRSA.

Welcome to talk about 98-97-5, If you have any questions, you can contact Liu, J; Zhang, GY; Zhang, Z; Li, B; Chai, F; Wang, Q; Zhou, ZD; Xu, LL; Wang, SK; Jin, Z; Tang, YZ or send Email.. COA of Formula: C5H4N2O2

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

SDS of cas: 98-97-5. In 2020 J MED CHEM published article about ANTIINFLAMMATORY DRUGS; IMMUNOPROTEASOME; DESIGN; CELLS; RISK in [Bhattarai, Deepak; Lee, Min Jae; Miller, Zachary; Kim, Kyung Bo] Univ Kentucky, Dept Pharmaceut Sci, Lexington, KY 40536 USA; [Baek, Ahruem; Baek, Yu Mi; Kim, Dong-Eun] Konkuk Univ, Dept Biosci & Biotechnol, Seoul 05029, South Korea; [Yeo, In Jun; Hong, Jin Tae] Chungbuk Natl Univ, Coll Pharm, Cheongju 28160, Chungbuk, South Korea; [Lee, Sukyeong] Baylor Coll Med, Verna & Marrs McLean Dept Biochem & Mol Biol, Houston, TX 77030 USA in 2020, Cited 43. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

The immunoproteasome (iP), an inducible proteasome variant harboring three immunosubunits, low molecular mass polypeptide-2 (LMP2), multicatalytic endopeptidase complex subunit-1, and low molecular mass polypeptide-7 (LMP7), is involved in multiple facets of inflammatory responses. We recently reported that YU102, a dual inhibitor of the iP subunit LMP2 and the constitutive proteasome catalytic subunit beta 1, ameliorates cognitive impairments in mouse models of Alzheimer’s disease (AD) independently of amyloid deposits. To investigate whether inhibition of LMP2 is sufficient to improve the cognitive functions of AD mice, here we prepared 37 YU102 analogues and identified a potent LMP2 inhibitor DB-310 (28) (IC50: 80.6 nM) with improved selectivity and permeability in cells overexpressing ABCB1 transporters. We show that DB-310 induces suppression of IL-1 alpha production in microglia cells and improves cognitive functions in the Tg2576 transgenic mouse model of AD. This study supports that inhibition of LMP2 is a promising therapeutic strategy for treatment of AD.

Welcome to talk about 98-97-5, If you have any questions, you can contact Bhattarai, D; Lee, MJ; Baek, A; Yeo, IJ; Miller, Z; Baek, YM; Lee, S; Kim, DE; Hong, JT; Kim, KB or send Email.. SDS of cas: 98-97-5

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Authors Dumpala, RMR; Boda, A; Kumar, P; Rawat, N; Ali, SM in AMER CHEMICAL SOC published article about MONOCARBOXYLATE-N-OXIDES; LIQUID-LIQUID-EXTRACTION; 2-PYRAZINECARBOXYLIC ACID; THEORETICAL INSIGHTS; LUMINESCENCE; SEPARATION; EUROPIUM(III); EU3+; LANTHANIDES; SELECTIVITY in [Dumpala, Rama Mohana Rao; Rawat, Neetika] Bhabha Atom Res Ctr, Radioanalyt Chem Div, Mumbai 400085, Maharashtra, India; [Boda, Anil; Ali, Sk. Musharaf] Bhabha Atom Res Ctr, Chem Engn Div, Mumbai 400085, Maharashtra, India; [Kumar, Pranaw] Bhabha Atom Res Ctr, Fuel Chem Div, Mumbai 400085, Maharashtra, India in 2019, Cited 52. Safety of Pyrazine-2-carboxylic acid. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

The denticity, flexibility, and steric hindrance of the ligand are key factors in deciding the mode and number of coordination around a metal ion on complex formation. The thermodynamic aspects of lanthanide complexation with various multidentate ligands provides a significant insight into understand the coordination chemistry of lanthanides in framing the relevant metal organic networks for the applications in biological, biochemical and medical aspects. The pyrazine carboxylic acids are known to form many structurally important complexes and further can form chelates with coordination number of eight for europium in which more water molecules can be knocked out from the primary coordination sphere than demanded by denticity of the ligand. The present studies aimed at ESI-MS characterization and determination of the thermodynamic parameters (log beta, Delta G, Delta H, and Delta S), luminescence properties of europium complexes with pyrazine-2-carboxylate and pyrazine-2,3-dicarboxylate in aqueous solutions by experiment as well as theory. Time resolved luminescence spectroscopy supported by DFT calculations are carried out to optimize the stable geometries of the complexes with various modes of binding and coordination. Furthermore, the thermodynamic parameters estimated theoretically have been used to trace the path of complex formation.

Welcome to talk about 98-97-5, If you have any questions, you can contact Dumpala, RMR; Boda, A; Kumar, P; Rawat, N; Ali, SM or send Email.. Safety of Pyrazine-2-carboxylic acid

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

I found the field of Life Sciences & Biomedicine – Other Topics very interesting. Saw the article Mechanistic analysis of A46V, H57Y, and D129N in pyrazinamidase associated with pyrazinamide resistance published in 2020. Quality Control of Pyrazine-2-carboxylic acid, Reprint Addresses Wei, DQ (corresponding author), Shanghai Jiao Tong Univ, State Key Lab Microbial Metab, Sch Life Sci & Biotechnol, Minist Educ, Shanghai 200240, Peoples R China.; Wei, DQ (corresponding author), Shanghai Jiao Tong Univ, Joint Lab Int Cooperat Metab & Dev Sci, Minist Educ, Shanghai 200240, Peoples R China.; Wei, DQ (corresponding author), Peng Cheng Lab, Vanke Cloud City Phase 1 Bldg 8,Xili St, Shenzhen 518055, Guangdong, Peoples R China.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Pyrazinamide (PZA) is a component of first-line drugs, active against latent Mycobacterium tuberculosis (MTB) isolates. The prodrug is activated into the active form, pyrazinoic acid (POA) via pncA gene-encoded pyrazinamidase (PZase). Mutations in pncA have been reported, most commonly responsible for PZA-resistance in more than 70% of the resistant cases. In our previous study, we detected many mutations in PZase among PZA-resistance MTB isolates including A46V, H71Y, and D129N. The current study was aimed to investigate the molecular mechanism of PZA-resistance behind mutants (MTs) A46V, H71Y, and D129N in comparison with the wild type (WT) through molecular dynamic (MD) simulation. MTB positive samples were subjected to PZA drug susceptibility testing (DST) against critical concentration (100ug/ml). The resistant samples were subjected to pncA sequencing. Thirty-six various mutations have been observed in the coding region of pncA of PZA-resistant isolates (GenBank accession No. MH461111) including A46V, H71Y, and D129N. The post-simulation analysis revealed a significant variation in MTs structural dynamics as compared to the WT. Root means square deviations (RMSD) and Root means square fluctuation (RMSF) has been found in variation between WT and MTs. Folding effect and pocket volume were altered in MTs when compared with WT. Geometric matching supports the effect of mutation A46V, H71Y, and D129N on PZase structure that may have an insight effect on PZase dynamics, making them vulnerable to convert pro-PZA into active form, POA. In conclusion, the current analyses will provide useful information behind PZA-resistance for better management of drug-resistant TB. (C) 2020 The Author(s). Published by Elsevier B.V. on behalf of King Saud University.

Quality Control of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Khan, MT; Chinnasamy, S; Cui, ZL; Irfan, M; Wei, DQ or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

An article Controllable luminescent behaviors with pyrazine and benzimidazole groups: Syntheses, crystal structures and properties WOS:000505108100018 published article about BIOLOGICAL EVALUATION; ORGANIC FRAMEWORKS; COMPLEXES; ANTICANCER; POLYMERS; DERIVATIVES; COPPER; DRUGS; PHOTOLUMINESCENCE; HETEROCYCLES in [Wang, Yong-Tao; Wu, Yu-Song; Tang, Gui-Mei] Qilu Univ Technol, Shandong Acad Sci, Dept Chem Engn, Jinan 250353, Shandong, Peoples R China in 2019, Cited 103. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Computed Properties of C5H4N2O2

A set of new salts containing benzimidazole and pyrazine groups, namely, [HPZBI]X-+(-) nH(2)O (X = Cl (n = 1) (1), NO3 (n = 1) (2), ClO4 (n = 0) (3) and H2PO4 (n = 0) (4)) [PZBI = 2-(pyrazin-2-yl)-1H-benzimidazole], were obtained by the reaction of PZBI and a set of inorganic acid, respectively. The emission maxima can be found at 444, 472, 471, 432 and 443 nm for PZBI and its compounds 1-4 in the solid state at room temperature, respectively. Compared with the free PZBI, the emission maxima of compounds 1-4 are obviously blue/red-shifted for 1-4, indicating that the emission maxima are relative to the intermolecular packing distances. Their photoluminescent lifetime and quantum yield are 1.10 ns and 24.5% for 1, 0.99 ns and 26.4% for 2, 0.94 ns and 21.65% for 3, 2.86 ns and 20.57% for 4, respectively. Compounds 1-4 were structurally characterized by X-ray single crystal diffraction, FT-IR, and UV-Vis spectra. Single crystal X-ray diffraction reveals that pi center dot center dot center dot pi packing interactions and a set of hydrogen bonds can be observed. The shortest distances of pi center dot center dot center dot pi stacking interactions are 3.613, 3.534, 3.731 and 3.492 angstrom in compounds 1-4, respectively. Additionally, the thermal stabilities of compounds 1-4 were investigated in detail.

Computed Properties of C5H4N2O2. Bye, fridends, I hope you can learn more about C5H4N2O2, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

An article Zirconium-Containing Organic-Inorganic Nanohybrid as a Highly Efficient Catalyst for the Selective Synthesis of Biomass-Derived 2,5-Dihydroxymethylfuran in Isopropanol WOS:000538735600030 published article about TRANSFER HYDROGENATION; LEVULINIC ACID; ELECTROCATALYTIC HYDROGENATION; REDUCTIVE ETHERIFICATION; FURFURYL ALCOHOL; CONVERSION; TRANSFORMATION; HMF; 2,5-BIS(HYDROXYMETHYL)FURAN; DERIVATIVES in [Hu, Lei; Liu, Su; Song, Jie; Jiang, Yetao; He, Aiyong; Xu, Jiaxing] Huaiyin Normal Univ, Jiangsu Collaborat Innovat Ctr Reg Modern Agr & E, Sch Chem & Chem Engn, Jiangsu Key Lab Biomass Based Energy & Enzyme Tec, Huaian 223300, Peoples R China in 2020, Cited 82. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Safety of Pyrazine-2-carboxylic acid

By the simple assembly of zirconium tetrachloride and diethylenetriaminepentaacetic acid (DTPA), a new acid-base bifunctional zirconium-containing organic-inorganic nanohybrid catalyst (Zr-DTPA) was successfully prepared in this work, and then used for the catalytic transfer hydrogenation (CTH) of biomass-derived 5-hydroxymethylfurfural (HMF) into 2,5-dihydroxymethylfuran (DHMF) using isopropanol as the in situ hydrogen donor and reaction solvent. Satisfactorily, 98.7% HMF conversion and 95.2% DHMF yield could be achieved in 4 h at a moderate reaction temperature of 140 degrees C. After systematic studies, this excellent catalytic activity was proved to be mainly ascribed to the synergistic effect of Lewis-acidic sites (Zr4+) and Lewis-basic sites (O2- and N) with higher strengths and contents. Meanwhile, Zr-DTPA could be readily separated by filtration, when it was repeatedly used 5 recycles, its catalytic activity was not obviously changed, demonstrating that Zr-DTPA had good heterogeneity and reusability. More importantly, Zr-DTPA could also be employed to effectively catalyze the CTH of 5-methylfurfural, furfural, levulinic acid, ethyl levulinate and cyclohexanone into the corresponding products with high yields, indicating that it showed a superior universality for the selective hydrogenation of various biomass-derived carbonyl compounds.Graphical Abstract

Safety of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Hu, L; Liu, S; Song, J; Jiang, YT; He, AY; Xu, JX or send Email.

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

An article Covalent docking modelling-based discovery of tripeptidyl epoxyketone proteasome inhibitors composed of aliphatic-heterocycles WOS:000458221400039 published article about BIOLOGICAL EVALUATION; MOLECULAR DOCKING; 20S PROTEASOME; DESIGN; DERIVATIVES; IDENTIFICATION; DEGRADATION; GENERATION; APOPTOSIS; MYELOMA in [Dong, Xiao-Wu; Zhang, Jian-Kang; Che, Jin-Xin; Liu, Tao; Hu, Yong-Zhou] Zhejiang Univ, ZJU ENS Joint Lab Med Chem, Zhejiang Prov Key Lab Anticanc Drug Res, Hangzhou Inst Innovat Med,Coll Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China; [Xu, Lei; Hu, Xiao-Bei; Sheng, Li; Gao, An-Hui; Li, Jia; Liu, Tao; Zhou, Yu-Bo] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; [Xu, Lei; Hu, Xiao-Bei; Sheng, Li; Gao, An-Hui; Li, Jia; Zhou, Yu-Bo] Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China; [Zhang, Jian-Kang] Zhejiang Univ City Coll, Sch Med, Hangzhou 310015, Zhejiang, Peoples R China; [Cheng, Gang] Zhejiang Chinese Med Univ, Coll Pharmaceut Sci, Hangzhou 311402, Zhejiang, Peoples R China in 2019, Cited 33. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Formula: C5H4N2O2

The potential of specific proteasome inhibitors to act as anti-cancer agents has attracted intensive investigations. The proteasome can be covalently inhibited by epoxyketone derivatives via a two-step reaction. Several computational approaches have been developed to mimic the covalent binding event. Compound 1 composed of a six-membered heterocyclic ring was designed by using covalent docking. With a possible different binding mode from the clinical compound Carfilzomib, it occupied the 55 pocket of 20S proteasome and showed favorable inhibitory activity. Subsequently optimization and evaluation were taken place. Among these compounds, 11h demonstrated extraordinary in vitro inhibitory activity and selectivity, and good in vivo proteasome inhibitory activity, a favorable pharmacokinetic profile and xenograft tumor inhibition. The possible binding pattern of compound 11h against proteasome was further fully explored via calculations, providing a theoretical basis for finding potent proteasome inhibitors. (C) 2018 Elsevier Masson SAS. All rights reserved.

Welcome to talk about 98-97-5, If you have any questions, you can contact Dong, XW; Zhang, JK; Xu, L; Che, JX; Cheng, G; Hu, XB; Sheng, L; Gao, AH; Li, J; Liu, T; Hu, YZ; Zhou, YB or send Email.. Formula: C5H4N2O2

Reference:
Patent; Chevron Research Company; US4732894; (1988); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem