Category: 98-97-5

An article Cell-Based Optimization of Covalent Reversible Ketoamide Inhibitors Bridging the Unprimed to the Primed Site of the Proteasome beta 5 Subunit WOS:000495744300001 published article about CRYSTAL-STRUCTURE; 20S PROTEASOME; ALPHA; EXPRESSION; BORTEZOMIB; SUBSTRATE; DOCKING in [Stubba, Daniel; Bensinger, Dennis; Steinbacher, Janika; Proskurjakov, Lilia; Gomez, Alvaro Salcedo; Schmitz, Katja; Schmidt, Boris] Tech Univ Darmstadt, Clemens Schoepf Inst Organ Chem & Biochem, Alarich Weiss Str 4, D-64287 Darmstadt, Germany; [Schmidt, Uwe; Roth, Stefan] Tech Univ Darmstadt, Dept Comp Sci, Visual Inference Lab, Huchschulstr 10, D-64289 Darmstadt, Germany in 2019, Cited 42. HPLC of Formula: C5H4N2O2. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

The ubiquitin-proteasome system (UPS) is an established therapeutic target for approved drugs to treat selected hematologic malignancies. While drug discovery targeting the UPS focuses on irreversibly binding epoxyketones and slowly-reversibly binding boronates, optimization of novel covalent-reversibly binding warheads remains largely unattended. We previously reported alpha-ketoamides to be a promising reversible lead motif, yet the cytotoxic activity required further optimization. This work focuses on the lead optimization of phenoxy-substituted alpha-ketoamides combining the structure-activity relationships from the primed and the non-primed site of the proteasome beta 5 subunit. Our optimization strategy is accompanied by molecular modeling, suggesting occupation of P1 ‘ by a 3-phenoxy group to increase beta 5 inhibition and cytotoxic activity in leukemia cell lines. Key compounds were further profiled for time-dependent inhibition of cellular substrate conversion. Furthermore, the alpha-ketoamide lead structure 27 does not affect escape response behavior in Danio rerio embryos, in contrast to bortezomib, which suggests increased target specificity.

Welcome to talk about 98-97-5, If you have any questions, you can contact Stubba, D; Bensinger, D; Steinbacher, J; Proskurjakov, L; Gomez, AS; Schmidt, U; Roth, S; Schmitz, K; Schmidt, B or send Email.. HPLC of Formula: C5H4N2O2

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

Recommanded Product: 98-97-5. Recently I am researching about MYCOBACTERIUM-TUBERCULOSIS; ANTIBACTERIAL ACTIVITY; RAMAN-SPECTROSCOPY; CONTROLLED-RELEASE; HYBRID MATERIALS; GRAPHITE; DELIVERY; NANOMATERIALS; CYTOTOXICITY; DOXORUBICIN, Saw an article supported by the EU (ERDF)European Commission [INFRANANOCHEM19/01.03.2009]; Romanian Government [INFRANANOCHEM19/01.03.2009]. Published in ELSEVIER SCIENCE BV in AMSTERDAM ,Authors: Tudos, M; Anghel, EM; Culita, DC; Somacescu, S; Calderon-Moreno, J; Tecuceanu, V; Dumitrascu, FD; Dracea, O; Popa, M; Marutescu, L; Bleotu, C; Curutiu, C; Chifiriuc, MC. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

In this work, we present a simple, two-stage method for the preparation of new and efficient antimicrobial hybrid systems, based on isoniazid and pyrazine-2-carbohydrazide tuberculostatic agents covalently linked to graphene oxide. In the first step, the carboxyl groups of graphene oxide are activated by transforming them into the corresponding acid chloride groups, which, in the second step, will react with the amino groups of the two drugs. Pyrazine-2-carbohydrazide was obtained from pyrazinoic acid and hydrazine hydrate and was confirmed by nuclear magnetic resonance spectroscopy. The materials have been characterized by elemental analysis, infrared spectroscopy, Raman spectroscopy, scanning electron microscopy, and X-ray photoelectron spectroscopy. Their antimicrobial activity was tested on mycobacterial (Mycobacterium terrae), as well as on Gram-negative bacteria (Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853), Gram-positive bacteria (Staphylococcus aureus ATCC 6538, Staphylococcus aureus ATCC 25923) and fungal (Candida albicans ATCC 10231), in planktonic and biofilm growth state. The biocompatibility of the tested compounds was assessed in vitro by live-dead fluorescence staining and flow cytometry. The results of this study have shown that the functionalization of graphene oxide with isoniazid and pyrazine-2-carbohydrazide both enhanced the anti-mycobacterial activity of the respective drugs and extended their antimicrobial spectrum towards other microbial strains, in planktonic and biofilm growth state, showing a promising potential for mitigating the impact of antimicrobial resistance and the deleterious effects of microbial biofilms. At the active tuberculostatic concentrations, the tested compounds exhibit very low cytotoxicity and do not interfere with the cellular cycle of Hep-2 cells. The flow cytometry and live/dead fluorescence staining proved that the tested compounds exhibit a microbicidal effect through induction of cellular lesions, consecutive to membrane depolarization.

Welcome to talk about 98-97-5, If you have any questions, you can contact Tudos, M; Anghel, EM; Culita, DC; Somacescu, S; Calderon-Moreno, J; Tecuceanu, V; Dumitrascu, FD; Dracea, O; Popa, M; Marutescu, L; Bleotu, C; Curutiu, C; Chifiriuc, MC or send Email.. Recommanded Product: 98-97-5

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

In 2019 J MATER SCI-MATER EL published article about DOPED POROUS CARBON; OXYGEN REDUCTION REACTION; ELECTRODE MATERIAL; ASSISTED SYNTHESIS; PERFORMANCE; GRAPHENE; ANODE; POLYACRYLONITRILE; ELECTROCATALYSTS; NANOPARTICLES in [Wang, Guanyi; Sun, Xingwei; Bai, Jie; Han, Limin] Inner Mongolia Univ Technol, Chem Engn Coll, Hohhot 010051, Peoples R China in 2019, Cited 49. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Quality Control of Pyrazine-2-carboxylic acid

In this paper, high-capacity supercapacitor material (Fe-Nx/CNFs) synthesized by electrospinning a metal complex in PAN/DMF solution with different temperatures was presented. Moreover, nitrogen doping (N-doping in short) has been used to tailor the properties of carbon nanofibers and rendered its potential use for capacitor as an effective way. The structural and morphological properties of the Fe-Nx/CNFs were fully characterized and the carbonation temperature of the Fe-Nx/CNFs precursor was optimized. Compared with the pure carbon nanofiber, the annealing temperature of optimized Fe-Nx/CNFs composites electrode material was 550 degrees C. Fabricating the binder-free iron-based electrode exhibited a higher capacitance of 629Fg(-1) at the current density of 1Ag(-1) in 4molL(-1) aqueous KOH electrolyte. Meanwhile, a cycling stability of 97% capacitance retention after cycling 2500at 5Ag(-1) was maintained. This outstanding performance was attributed to the formation of the Fe-N bond and N-doped carbon nanofibers that effectively facilitates electronic transport. Therefore, carbon nanofibers, wherein nitrogen-doped metal (iron) center, exhibited high performance as supercapacitors.

Quality Control of Pyrazine-2-carboxylic acid. 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 Alkylpyrazines from Coffee are Extensively Metabolized to Pyrazine Carboxylic Acids in the Human Body WOS:000476571400006 published article about 5-HYDROXYPYRAZINOIC ACID; NICOTINIC-ACID; RAT; CONSUMPTION; MECHANISM; PLASMA; URINE in [Kremer, Jonathan I.; Pickard, Stephanie; Stadlmair, Lara F.; Glass-Theis, Anika; Buckel, Leon; Bakuradze, Tamara; Eisenbrand, Gerhard; Richling, Elke] Tech Univ Kaiserslautern, Dept Chem, Div Food Chem & Toxicol, Erwin Schrodinger Str 52, D-67663 Kaiserslautern, Germany in 2019, Cited 33. Recommanded Product: Pyrazine-2-carboxylic acid. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Scope Coffee is a complex mixture of over 1000 compounds, including diverse heteroaromatic compounds such as alkylpyrazines. Little is known about the intake, metabolism, and bodily distribution of these compounds. Therefore, a human intervention study is conducted to investigate the excretion of alkylpyrazine metabolites in urine after the ingestion of brewed coffee containing alkylpyrazines. Methods and results After consuming a diet without heat-processed food, ten volunteers consumed 500 mL of freshly brewed coffee prepared from coffee pads, providing intakes of 2-methylpyrazine (2-MeP), 2,5-dimethylpyrazine (2,5-DMeP), and 2,6-dimethylpyrazine (2,6-DMeP) amounting to 17.2, 4.4, and 4.9 mu mol, respectively. These alkylpyrazines are metabolized into the corresponding pyrazine carboxylic acids, namely pyrazine-2-carboxylic acid (PA), 5-hydroxypyrazine-2-carboxylic acid (5-OHPA), 5-methylpyrazine-2-carboxylic acid (5-MePA), and 6-methylpyrazine-2-carboxylic acid (6-MePA). In total, 64% of the ingested 2-MeP is excreted as PA, as well as 26% as 5-OHPA, while 91% and 97% of the ingested 2,5-DMeP and 2,6-DMeP are recovered as 5-MePA and 6-MePA, respectively, in urine samples collected after coffee consumption. Conclusion This study provides evidence that alkylpyrazines are rapidly metabolized into the corresponding carboxylic acids and excreted via urine by humans, which is consistent with earlier rodent studies.

Welcome to talk about 98-97-5, If you have any questions, you can contact Kremer, JI; Pickard, S; Stadlmair, LF; Glass-Theis, A; Buckel, L; Bakuradze, T; Eisenbrand, G; Richling, E or send Email.. Recommanded Product: Pyrazine-2-carboxylic acid

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

Safety of Pyrazine-2-carboxylic acid. Authors Drozd, KV; Manin, AN; Voronin, AP; Perlovich, GL in ACADEMIC PRESS LTD- ELSEVIER SCIENCE LTD published article about in [Drozd, K., V; Manin, A. N.; Voronin, A. P.; Perlovich, G. L.] RAS, GA Krestov Inst Solut Chem, Ivanovo 153045, Russia in 2021, Cited 70. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

The thermophysical characteristics and decomposition of pyrazinoic (POA), dipicolinic (DPA), and quinolinic (QNA) acids have been studied by differential scanning calorimetry (DSC), thermogravimetric analysis (TG) and mass-spectrometry. The transpiration method has been used to measure the vapour pressures as a function of the POA, DPA or QNA temperature. It has been found that QNA remains thermally stable in the solid form up to the temperature of 367.15 K, and further heating causes its decarboxylation and irreversible conversion to nicotinic acid. The standard molar enthalpies, entropies, and Gibbs energies of sublimation for POA, DPA and QNA have been calculated. A comparative study of five calculation schemes for sublimation enthalpy estimation (periodic Density Functional Theory computations (DFT-D3), Quantum Theory of Atoms in Molecules (QTAIM), Gavezzotti’s Coulomb-London-Pauli model (CLP and PIXEL) and CrystalExplorer CE-B3LYP) has been conducted. The sublimation thermodynamic functions of the compounds studied by the correlation method have been estimated. When applied to the objects of this study, the method proved to be a quick, convenient and inexpensive way to evaluate the sublimation thermodynamic functions of molecular crystals using only the melting temperature of the compound. (C) 2020 Elsevier Ltd.

Safety of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Drozd, KV; Manin, AN; Voronin, AP; Perlovich, GL or send Email.

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

Stenger-Smith, J; Kamariza, M; Chakraborty, I; Ouattara, R; Bertozzi, CR; Mascharak, PK in [Stenger-Smith, Jenny; Chakraborty, Indranil; Ouattara, Ramatoulaye; Mascharak, Pradip K.] Univ Calif Santa Cruz, Dept Chem & Biochem, Santa Cruz, CA 95064 USA; [Kamariza, Mireille; Bertozzi, Carolyn R.] Stanford Univ, Dept Chem, Stanford, CA 94305 USA published Enhanced Bactericidal Effects of Pyrazinamide Toward Mycobacterium smegmatis and Mycobacterium tuberculosis upon Conjugation to a {Au(I)-triphenylphosphine}(+) Moiety in 2020, Cited 42. Product Details of 98-97-5. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

As part of the quest for new gold drugs, we have explored the efficacy of three gold complexes derived from the tuberculosis drug pyrazinamide (PZA), namely, the gold(I) complex [Au(PPh3)(PZA)]OTf (1, OTf = trifluoromethanesulfonate) and two gold(III) complexes [Au(PZA)Cl-2] (2) and [Au(PZO)Cl-2] (3, PZO = pyrazinoic acid, the metabolic product of PZA) against two mycobacteria, Mycobacterium tuberculosis and Mycobacterium smegmatis. Only complex 1 with the {Au(PPh3)}(+) moiety exhibits significant bactericidal activity against both strains. In the presence of thiols, 1 gives rise to free PZA and {Au(PPh3)}-thiol polymeric species. A combination of PZA and the {Au(PPh3)}-thiol polymeric species appears to lead to enhanced efficacy of 1 against M. tuberculosis.

Welcome to talk about 98-97-5, If you have any questions, you can contact Stenger-Smith, J; Kamariza, M; Chakraborty, I; Ouattara, R; Bertozzi, CR; Mascharak, PK or send Email.. Product Details of 98-97-5

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

An article Amidation Reaction of Quinoline-3-carboxylic Acids with Tetraalkylthiuram Disulfides under Simple Conditions: A facile Synthesis of Quinoline-3-carboxamides WOS:000577748400001 published article about CROSS-COUPLING REACTIONS; CARBOXYLIC-ACIDS; QUINOLINE; SITE; DERIVATIVES; CARBONYLATION; COMPLEXES; RECEPTOR in [Hu, Jingyan; Ye, Xiefeng; Hao, Shuai; Zhao, Qianrui; Zhao, Mingqin; Wei, Yuewei; Wu, Zhiyong; Ji, Xiaoming] Henan Agr Univ, Flavors & Fragrance Engn & Technol Res Ctr Henan, Coll Tobacco Sci, 95 Wenhua Rd, Zhengzhou 450002, Peoples R China; [Wang, Na] China Tobacco Hubei Ind Co Ltd, Ctr Technol, 1355 Jinshan Rd, Wuhan 430040, Peoples R China in 2020, Cited 46. 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

A highly efficient and simple procedure for the synthesis quinoline-3-carboxamides and their analogues via amidation reaction of quinoline-3-carboxylic acids with tetraalkylthiuram disulfides has been developed. The reaction proceeds efficiently under simple reaction conditions and features the generality of broad scope of substrates with good yields. This protocol provides a convenient procedure for the synthesis of various aza-heteroaromatic carboxamides, which is of pharmaceutical interest.

SDS of cas: 98-97-5. 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

I found the field of Thermodynamics; Chemistry very interesting. Saw the article Mechanochemical synthesis, characterization and thermal study of new cocrystals of ciprofloxacin with pyrazinoic acid and p-aminobenzoic acid published in 2020. Name: Pyrazine-2-carboxylic acid, Reprint Addresses Caires, F (corresponding author), Sao Paulo State Univ, Inst Chem, UNESP, Araraquara, Brazil.; Caires, F (corresponding author), Sao Paulo State Univ, Sch Sci, UNESP, Bauru, Brazil.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Novel cocrystals of ciprofloxacin with pyrazinoic acid and p-aminobenzoic acid in the 1:1 stoichiometric ratio were obtained by the mechanochemical method, under conditions of liquid-assisted grinding (LAG/ethanol) and neat grinding. They were characterized by powder X-ray diffractometry, infrared spectroscopy, simultaneous thermogravimetry, differential thermal analysis, differential scanning calorimetry (DSC) and DSC-Microscopy system. The results confirmed the successful synthesis of the cocrystals and indicated the functional groups responsible for the formation of the new supramolecular synthons. In addition, from the thermal analysis, it was possible to evaluate the thermal stability, composition, crystallization processes during heating, polymorphic transitions and construct the binary phase diagrams.

Welcome to talk about 98-97-5, If you have any questions, you can contact de Almeida, AC; Ferreira, PO; Torquetti, C; Ekawa, B; Carvalho, ACS; dos Santos, EC; Caires, F or send Email.. Name: Pyrazine-2-carboxylic acid

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

An article Novel pyrazine based anti-tubercular agents: Design, synthesis, biological evaluation and in silico studies WOS:000516796900043 published article about MYCOBACTERIUM-TUBERCULOSIS; ANTIMYCOBACTERIAL ACTIVITY; ACID HYDRAZONES; DERIVATIVES; RESISTANCE; DOCKING; DRUGS; GRANULOCYTES; INHIBITORS; PREDICTION in [Hassan, Nayera W.; Saudi, Manal N.; Abdel-Ghany, Yasser S.; Ismail, Azza; Elzahhar, Perihan A.; El-Hawash, Soad A.] Alexandria Univ, Fac Pharm, Dept Pharmaceut Chem, Alexandria 21521, Egypt; [Sriram, Dharmarajan] Birla Inst Technol & Sci Pilani, Med Chem & Drug Discovery Res Lab, Pharm Grp, Hyderabad Campus, Jawahar Nagar 500078, Telangana, India; [Nassra, Rasha] Alexandria Univ, Fac Med, Dept Med Biochem, Alexandria, Egypt; [Abdel-Aziz, Marwa M.] Al Azhar Univ, Reg Ctr Mycol & Biotechnol, Cairo 11759, Egypt in 2020, Cited 84. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Product Details of 98-97-5

TB continues to be a leading health threat despite the availability of powerful anti-TB drugs. We report herein the design and synthesis of various hybrid molecules comprising pyrazine scaffold and various formerly identified anti-mycobacterial moieties. Thirty-one compounds were screened in vitro for their activity against Mycobacterium tuberculosis H37Rv strain using MABA assay. The results revealed that six compounds (8a, 8b, 8c, 8d, 14b and 18) displayed significant activity against Mtb with MIC values <= 6.25 mu g/ml versus 6.25 mu g/ml for pyrazinamide. The most active compounds were then assessed for their in vitro cytotoxicity against PBMC normal cell line using MTT assay and showed SI > 200. Several in silico studies have been carried out for target fishing of the novel compounds such as shape-based similarity, pharmacophore mapping and inverse docking. Based on this multi-step target fishing study, we suggest that pantothenate synthetase could be the possible target responsible for the action of these compounds. The most active compounds were then successfully docked into the active site of pantothenate synthetase enzyme with favorable binding interactions. In addition, in silico prediction of physicochemical, ADMET and drug-like properties were also determined indicating that compounds 8b, 8c and 8d are promising candidates for the development of new anti-TB agents with enhanced activity and better safety profile.

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.. Product Details of 98-97-5

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

Formula: C5H4N2O2. Authors Swiderski, G; Kalinowska, M; Jablonska-Trypuc, A; Wolejko, E; Wydro, U; Lyszczek, R; Rusinek, I; Lewandowski, W in ELSEVIER published article about in [Swiderski, Grzegorz; Kalinowska, Monika; Jablonska-Trypuc, Agata; Wolejko, Elzbieta; Wydro, Urszula; Lewandowski, Wlodzimierz] Bialystok Tech Univ, Dept Chem Biol & Biotechnol, Wiejska 45E St, PL-15351 Bialystok, Poland; [Lyszczek, Renata; Rusinek, Iwona] UMCS, Dept Gen & Coordinat Chem, MC Sklodowska Sq 2, PL-20031 Lublin, Poland in 2021, Cited 50. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

Diazinecarboxylic acids (pyridazine-3-carboxylic, pyridazine-4-carboxylic, pyrimidine-2-carboxylic, pyrimidine-4-carboxylic, pyrimidine-5-carboxylic and pyrazine-2-carboxylic acids) were characterized by means of spectroscopic (FT-Raman, FTIR, UV, (HNMR)-H-1, (CNMR)-C-13) and thermogravimetric analysis as well as antimicrobial and cytotoxic tests. The structures of diazinecarboxylic acids were calculated by the DFT method (B3LYP/6-311G(d, p). For the most stable conformers, the energy of HOMO and LUMO molecular orbitals, the geometric (HOMA, GEO, EN, I6) and magnetic (NICS) aromaticity indices, NBO electronic charge distribution, sEDA and pEDA indexes, Wiberg Bond Order, Wiberg Index and theoretical IR and NMR spectra have been calculated. The energies of protonating and deprotonating acids were also calculated. The effect of the nitrogen heteroatom position in the aromatic ring in relation to the position of the carboxyl group on the electronic charge distribution, thermal stability, antimicrobial and cytotoxicity activities of the examined acids was determined. Antimicrobial activity of tested acids against of Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosaand Candida albicanswas calculated based on MTT colorimetric assay (MCA). The cytotocic effect of diazynecarboxylic acids was examined in A375 melanoma cell line and DLD-1 cell line. A biplot analysis was performed in order to determine the correlations between selected parameters of the tested compounds and relative cell viability of E. coli, B. subtilis, P. aeruginosa, C. albicans, A375 and DLD-1 cell lines. Thermal behaviour of all investigated carboxylic acids was investigated using thermogravimetry (TG) and differential scanning calorimetry (DSC) techniques in flowing air atmosphere. All compounds are stable in room temperature. (C) 2021 Elsevier B.V. All rights reserved.

Welcome to talk about 98-97-5, If you have any questions, you can contact Swiderski, G; Kalinowska, M; Jablonska-Trypuc, A; Wolejko, E; Wydro, U; Lyszczek, R; Rusinek, I; Lewandowski, W or send Email.. Formula: C5H4N2O2

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