Category: Pyrazines

Name: Pyrazine-2-carboxylic acid. Authors Korff, M; Imberg, L; Will, JM; Buckreiss, N; Kalinina, SA; Wenzel, BM; Kastner, GA; Daniliuc, CG; Barth, M; Ovsepyan, RA; Butov, KR; Humpf, HU; Lehr, M; Panteleev, MA; Poso, A; Karst, U; Steinmetzer, T; Bendas, G; Kalinin, DV in AMER CHEMICAL SOC published article about in [Korff, Marvin; Imberg, Lukas; Kastner, Gregor A.; Barth, Maximilian; Lehr, Matthias; Kalinin, Dmitrii, V] Univ Munster, Inst Pharmaceut & Med Chem, D-48149 Munster, Germany; [Will, Jonas M.; Karst, Uwe] Univ Munster, Inst Inorgan & Analyt Chem, D-48149 Munster, Germany; [Bueckreiss, Nico; Bendas, Gerd] Univ Bonn, Pharmaceut Inst, D-53121 Bonn, Germany; [Kalinina, Svetlana A.; Humpf, Hans-Ulrich] Univ Munster, Inst Food Chem, D-48149 Munster, Germany; [Wenzel, Benjamin M.; Steinmetzer, Torsten] Philipps Univ Marburg, Inst Pharmaceut Chem, Dept Pharm, D-35032 Marburg, Germany; [Daniliuc, Constantin G.] Univ Munster, Inst Organ Chem, D-48149 Munster, Germany; [Ovsepyan, Ruzanna A.; Butov, Kirill R.; Panteleev, Mikhail A.] Dmitriy Rogachev Natl Med Res Ctr Pediat Hematol, Lab Translat Med, Moscow 117997, Russia; [Ovsepyan, Ruzanna A.; Butov, Kirill R.; Panteleev, Mikhail A.] Russian Acad Sci, Ctr Theoret Problems Physicochem Pharmacol, Moscow 119991, Russia; [Panteleev, Mikhail A.] Lomonosov Moscow State Univ, Fac Phys, Moscow 119991, Russia; [Panteleev, Mikhail A.] Moscow Inst Phys & Technol, Fac Biol & Med Phys, Dolgoprudnyi 141700, Russia; [Poso, Antti] Univ Eastern Finland, Fac Hlth Sci, Sch Pharm, Kuopio 70211, Finland; [Poso, Antti] Univ Hosp Tubingen, Dept Internal Med 8, D-72076 Tubingen, Germany in 2020, Cited 75. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5

We herein report the conventional and microscale parallel synthesis of selective inhibitors of human blood coagulation factor XIIa and thrombin exhibiting a 1,2,4-triazol-5-amine scaffold. Structural variations of this scaffold allowed identifying derivative 21i, a potent 29 nM inhibitor of FXIIa, with improved selectivity over other tested serine proteases and also finding compound 21m with 27 nM inhibitory activity toward thrombin. For the first time, acylated 1,2,4-triazol-5-amines were proved to have anticoagulant properties and the ability to affect thrombin- and cancer-cell-induced platelet aggregation. Performed mass spectrometric analysis and molecular modeling allowed us to discover previously unknown interactions between the synthesized inhibitors and the active site of FXIIa, which uncovered the mechanistic details of FXIIa inhibition. Synthesized compounds represent a promising starting point for the development of novel antithrombotic drugs or chemical tools for studying the role of FXIIa and thrombin in physiological and pathological processes.

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

Recommanded Product: Pyrazine-2-carboxylic acid. In 2020 CHEMISTRYSELECT published article about HELICOBACTER-PYLORI; BIOISOSTERIC TRANSFORMATIONS; TRIPLE THERAPY; PATHOGENESIS; METAANALYSIS; OXADIAZOLES; PREDICTION in [Azizian, Homa] Iran Univ Med Sci, Sch Pharm, Dept Med Chem, Int Campus, Tehran, Iran; [Esmailnejad, Atefeh; Fathi Vavsari, Vaezeh; Balalaie, Saeed] KN Toosi Univ Technol, Peptide Chem Res Ctr, POB 15875-4416, Tehran, Iran; [Mahernia, Shabnam; Amanlou, Massoud] Univ Tehran Med Sci, TIPS, Drug Design & Dev Res Ctr, Tehran, Iran; [Balalaie, Saeed] Kermanshah Univ Med Sci, Med Biol Res Ctr, Kermanshah, Iran in 2020, Cited 42. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

A number of pantoprazole derivatives were synthesized and screened for their urease inhibitory properties. Some of them showed potent inhibitions against jack bean urease. All compounds showed varying degree of IC50 in the range of 25.85 to 181 mu Mol as compared to standard acetohydroxamic acid (AHA) (100 +/- 2.02 mu Mol). Derivatives bearing 5-aryl-1,3,4-oxadiazole ring substitutions (aryl= pyrazyl, pyridyl and phenyl) were found to be more potent inhibitors than AHA and pantoprazole. The most promising compound, 2-((3,4-dimethoxypyridin-2-yl)methylthio)-5-(pyrazin-2-yl)-1,3,4-oxadiazole 12, with IC50 value of 25.85 +/- 1.21 showed remarkable urease inhibition activity. In silico molecular modeling investigation performed to rationalize the possible binding interaction and ADME properties of compounds over the active site of urease enzyme. The induced fit docking study showed that compound 12 interacted with conserved residues His593 and Arg609 located at the mouth of the urease active site flap and are essential for enzyme catalytic activity. These target compounds could be further studied as a lead skeleton for discovery of novel urease inhibitors.

Recommanded Product: Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Azizian, H; Esmailnejad, A; Vavsari, VF; Mahernia, S; Amanlou, M; Balalaie, S or send Email.

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

COA of Formula: C5H4N2O2. In 2020 MED CHEM RES published article about ANTIMYCOBACTERIAL EVALUATION; ONE-POT; ESTERIFICATION; ESTERS; AMIDES; AMINES in [Wati, First A.; Adyarini, Prisna U.; Fatmawati, Sri; Santoso, Mardi] Inst Teknol Sepuluh Nopember, Fac Sci, Dept Chem, Kampus ITS Sukolilo, Surabaya 60111, Indonesia in 2020, Cited 24. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5.

The Yamaguchi reaction is widely and generally applied to synthesize esters and lactones. It involves 2,4,6-trichlorobenzoyl chloride as the Yamaguchi reagent, 4-dimethylaminopyridine, and triethylamine. Pyrazinamide is a crucial first-line drug for tuberculosis treatment, therefore their analogues are interesting in organic synthesis. In general, the synthesis pyrazinamide analogues involve reaction of pyrazine-2-carboxylic acids with thionyl chloride to yield the corresponding acyl chlorides, which on treatment with amines gave pyrazine-2-carboxamides. However, thionyl chloride is listed under the Chemical Weapons Convention and releases toxic sulfur oxide when react with carboxylic acid. We successfully synthesized series of pyrazinamide analogues using the Yamaguchi reaction. The synthesis involved reaction of pyrazine-2-carboxylic acid with various aliphatic and aromatic amines in the presence of Yamaguchi reagent and 4-dimethylaminopyridine. The yield of the pyrazine-2-carboxamides and the reaction time depended on the type of the amine (aliphatic vs aromatic), substitution pattern, and number of substituents on the aromatic amines.N-(4-chlorophenyl)pyrazine-2-carboxamides can be prepared by this method in 81% yield;N-(2-ethylhexyl)pyrazine-2-carboxamide andN-(4-fluorobenzyl)pyrazine-2-carboxamide showed the best activity againstMycobacterium tuberculosisH37Rv (<6.25 mu g/mL). This result could lead to find more active pyrazinamide analogues. Welcome to talk about 98-97-5, If you have any questions, you can contact Wati, FA; Adyarini, PU; Fatmawati, S; Santoso, M or send Email.. COA of Formula: C5H4N2O2

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

Recently I am researching about 5-HYDROXYPYRAZINOIC ACID; NICOTINIC-ACID; RAT; CONSUMPTION; MECHANISM; PLASMA; URINE, Saw an article supported by the German Federal Ministry of Education and Research (BMBF)Federal Ministry of Education & Research (BMBF) [0315692]. Recommanded Product: Pyrazine-2-carboxylic acid. Published in WILEY in HOBOKEN ,Authors: Kremer, JI; Pickard, S; Stadlmair, LF; Glass-Theis, A; Buckel, L; Bakuradze, T; Eisenbrand, G; Richling, E. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

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.

Recommanded Product: 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

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Anti-Mycobacterial Peroxides: A New Class of Agents for Development Against Tuberculosis published in 2020. Formula: C5H4N2O2, Reprint Addresses Parkinson, CJ (corresponding author), Charles Sturt Univ, Sch Biomed Sci, Orange, NSW 2800, Australia.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

Background: With few exceptions, existing tuberculosis drugs were developed many years ago and resistance profiles have emerged. This has created a need for new drugs with discrete modes of action. There is evidence that tuberculosis (like other bacteria) is susceptible to oxidative pressure and this has yet to be properly utilised as a therapeutic approach in a manner similar to that which has proven highly successful in malaria therapy. Objective: To develop an alternative approach to the incorporation of bacterial siderophores that results in the creation of antitubercular peroxidic leads for subsequent development as novel agents against tuberculosis. Methods: Eight novel peroxides were prepared and the antitubercular activity (H(37)Rv) was compared to existing artemisinin derivatives in vitro. The potential for toxicity was evaluated against the L6 rat skeletal myoblast and HeLa cervical cancer lines in vitro. Results: The addition of a pyrimidinyl residue to an artemisinin or, preferably, a tetraoxane peroxidic structure results in antitubercular activity in vitro. The same effect is not observed in the absence of the pyrimidine or with other heteroaromatic substituents. Conclusion: The incorporation of a pyrimidinyl residue adjacent to the peroxidic function in an organic peroxide results in anti-tubercular activity in an otherwise inactive peroxidic compound. This will be a useful approach for creating oxidative drugs to target tuberculosis.

Formula: 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

Safety of Pyrazine-2-carboxylic acid. I found the field of Chemistry very interesting. Saw the article Pantoprazole Derivatives: Synthesis, Urease Inhibition Assay and In Silico Molecular Modeling Studies published in 2020, Reprint Addresses Balalaie, S (corresponding author), KN Toosi Univ Technol, Peptide Chem Res Ctr, POB 15875-4416, Tehran, Iran.; Balalaie, S (corresponding author), Kermanshah Univ Med Sci, Med Biol Res Ctr, Kermanshah, Iran.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid.

A number of pantoprazole derivatives were synthesized and screened for their urease inhibitory properties. Some of them showed potent inhibitions against jack bean urease. All compounds showed varying degree of IC50 in the range of 25.85 to 181 mu Mol as compared to standard acetohydroxamic acid (AHA) (100 +/- 2.02 mu Mol). Derivatives bearing 5-aryl-1,3,4-oxadiazole ring substitutions (aryl= pyrazyl, pyridyl and phenyl) were found to be more potent inhibitors than AHA and pantoprazole. The most promising compound, 2-((3,4-dimethoxypyridin-2-yl)methylthio)-5-(pyrazin-2-yl)-1,3,4-oxadiazole 12, with IC50 value of 25.85 +/- 1.21 showed remarkable urease inhibition activity. In silico molecular modeling investigation performed to rationalize the possible binding interaction and ADME properties of compounds over the active site of urease enzyme. The induced fit docking study showed that compound 12 interacted with conserved residues His593 and Arg609 located at the mouth of the urease active site flap and are essential for enzyme catalytic activity. These target compounds could be further studied as a lead skeleton for discovery of novel urease inhibitors.

Safety 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

I found the field of Pharmacology & Pharmacy; Chemistry very interesting. Saw the article Synthesis of novel of 2, 5-disubstituted 1, 3, 4-oxadiazole derivatives and their in vitro anti-inflammatory, anti-oxidant evaluation, and molecular docking study published in 2020. Recommanded Product: 98-97-5, Reprint Addresses Ghanwat, AA (corresponding author), Solapur Univ, Sch Chem Sci, Chem Res Lab, Solapur 413255, India.. The CAS is 98-97-5. Through research, I have a further understanding and discovery of Pyrazine-2-carboxylic acid

A series of novel 2, 5-disubstituted 1, 3, 4-Oxadiazole derivatives as a potential anti-inflammatory, and antioxidant agent were synthesized via cyclisation. Hydrazide molecule treated with substituted acids in the presence of phosphorus oxychloride (POCl3) as an efficient reagent as well as solvent by conventional method with shorter reaction time and excellent yield. The newly synthesized 1, 3, 4-oxadiazole derivatives exhibited excellent to good anti-inflammatory and anti-oxidant activities compaired to the standard drugs. Molecular docking study on the crucial anti-inflammatory target-cyclooxygenase-2 (COX-2) revealed the ability of the scaffold to correctly recognize the active site and achieve significant bonded and non-bonded interactions with key residues therein. This study could identify potential compounds which can be pertinent starting points for structure-based drug design to obtain newer anti-inflammatory agents.

Recommanded Product: 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

In 2020 BIOORG MED CHEM LETT published article about ANTI-TUBERCULAR ACTIVITY; DESIGN; HYBRIDS; 1,2,3-TRIAZOLE; HYBRIDIZATION; ANTIMYCOBACTERIAL; DIARYLQUINOLINE in [Reddyrajula, Rajkumar; Dalimba, Udayakumar] Natl Inst Technol Karnataka, Dept Chem, Organ Chem Lab, Mangalore 575025, India in 2020, Cited 38. The Name is Pyrazine-2-carboxylic acid. Through research, I have a further understanding and discovery of 98-97-5. Application In Synthesis of Pyrazine-2-carboxylic acid

Tuberculosis remains as a major public health risk which causes the highest mortality rate globally and an improved regimen is required to treat the drug-resistant strains. Pyrazinamide is a first-line antitubercular drug used in combination therapy with other anti-TB drugs. Herein, we describe the modification of pyrazinamide structure using bioisosterism and rational approaches by incorporating the 1,2,3-triazole moiety. Three sets of pyrazine-1,2,3-triazoles (3a-o, 5a-o and 9a-l) are designed, synthesized and evaluated for their in vitro inhibitory potency against mycobacterium tuberculosis H(37)Rv. The pyrazine-1,2,3-triazoles synthesized through the bioisosteric modification displayed improved activity as compared to rationally modified pyrazine-1,2,3-triazoles. Among 42 title compounds, seven derivatives demonstrated significant anti-tubercular activity with the MIC of 1.56 mu g/mL, which are two-fold more potent than the parent compound pyrazinamide. Further, the synthesized pyrazinamide analogs demonstrated moderate inhibition activity against several bacterial strains and possessed an acceptable in vitro cytotoxicity profile as well. Additionally, the activity profile of pyrazine-1,2,3-triazoles was validated by performing the molecular docking studies against the Inh A enzyme. Furthermore, in silico ADME prediction revealed good oral bioavailability for the potent molecules.

Application In Synthesis of Pyrazine-2-carboxylic acid. Welcome to talk about 98-97-5, If you have any questions, you can contact Reddyrajula, R; Dalimba, U or send Email.

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

Authors Dumpala, RMR; Das, SK; Ali, M; Boda, A; Kumar, P; Rawat, N; Kumar, A; Ali, SM in PERGAMON-ELSEVIER SCIENCE LTD published article about in [Dumpala, Rama Mohana Rao; Rawat, Neetika] Bhabha Atom Res Ctr, Radiochem Div, Mumbai 400094, Maharashtra, India; [Das, Sourav Kumar; Ali, Manjoor; Kumar, Amit] Bhabha Atom Res Ctr, Radiat Biol & Hlth Sci Div, Mumbai 400094, Maharashtra, India; [Boda, Anil; Ali, Sk Musharaf] Bhabha Atom Res Ctr, Chem Engn Div, Mumbai 400094, Maharashtra, India; [Kumar, Pranaw] Bhabha Atom Res Ctr, Fuel Chem Div, Mumbai 400094, Maharashtra, India in 2021, Cited 78. 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

Thorium (Th) exposure to the human beings is a radiochemical hazard and the chelation therapy by suitable drugs is the major prevention approach to deal with. The present studies aimed at usage of pyrazinoic acid (PCA), which is a prodrug to treat tuberculosis, for its usage as decorporating agent for thorium from human body. The present studies provide a comprehensive knowledge on the chemical interaction and biological efficacy of pyrazinoic acid (PCA) for decorporation of Thorium from the human body. The thermodynamic parameters for Th-PCA speciation are determined by both experiment and theory. The potentiometric data analysis and Electro-Spray Ionization Mass Spectrometry (ESI-MS) studies revealed the formation of MLi (i = 1-4) species with the decrease in stepwise stability constants. All the species formations are endothermic reactions and are predominantly entropy-driven. Biological experiments using human erythrocytes, whole blood and normal human lung cells showed cytocompatibility and decorporation ability of PCA for Thorium. Density functional calculations have been carried out to get insights on interaction process at molecular level. The experimental results and theoretical predictions found to be in line with each other. Present findings on complexation of Th by PCA and its evaluation in human cells and blood would further motivate determination of its safety levels and decorporation efficacy in animal models. (C) 2021 Elsevier Ltd. All rights reserved.

Recommanded Product: 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 A chromone based Schiff base: An efficient colorimetric sensor for specific detection of Cu (II) ion in real water samples WOS:000609153400003 published article about FLUORESCENT DETECTION; CHEMOSENSOR; PROBE; COPPER; PRECONCENTRATION; FE3+; SITE in [Tomer, Nisha; Goel, Apurva; Malhotra, Rajesh] Guru Jambheshwar Univ Sci & Technol, Dept Chem, Hisar 125001, Haryana, India; [Ghule, Vikas D.] Natl Inst Technol, Dept Chem, Kurukshetra 136119, Haryana, India in 2021, Cited 45. 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

A new chromone based Schiff base ligand L was synthesized by the condensation of 3-formyl chromone and pyrazine-2-carbohydrazide as a colorimetric probe to detect Cu (II) ions selectively. An instant visual colour change from colourless to yellow was obtained on addition of Cu2+ ions to the probe L solution, while other metal ions found ineffective. The ligand L was characterized by H-1 NMR, FTIR and HRMS spectral techniques. UV-Visible spectroscopic technique was used to study the sensing ability of probe L for copper ions above other metal ions. The Job’s plot obtained from absorption studies and HRMS data confirmed that the Cu2+ ions bind with ligand L in 1:1 stoichiometric ratio. DFT computations were also supported the binding framework between L and Cu (II) ions. The LOD value and the association constant were obtained 3.9 x 10(-7) M and 2.3 x 10(5) M-1 respectively, via Benesi-Hildebrand equation. Selectivity of L towards Cu2+ ions was also studied and it was found that the probe L worked specifically for copper ions without any considerable influence of other intruding metal ions. In addition, in real water samples, the ligand L was fully implemented for identification and quantification of Cu2+ ions. (C) 2020 Elsevier B.V. All rights reserved.

Welcome to talk about 98-97-5, If you have any questions, you can contact Tomer, N; Goel, A; Ghule, VD; Malhotra, R or send Email.. Safety of Pyrazine-2-carboxylic acid

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